Asian Journal of Organic Chemistry最新文献

{"title":"Chemoselective Synthesis of Quinazoline and Quinazolinone Derivatives via NH4I‐Mediated Oxidative Annulation Under Metal‐ and Additive‐Free Conditions","authors":"Yongzhen Li,&nbsp;Yajing Liu,&nbsp;Jiajin Luo,&nbsp;Zhiwei Xi,&nbsp;Shuo‐Wen Wang,&nbsp;Ji‐Kai Wen,&nbsp;Shi Tang","doi":"10.1002/ajoc.70527","DOIUrl":"10.1002/ajoc.70527","url":null,"abstract":"<div><div>Owing to the structural importance and synthetic value of quinazoline and quinazolinone scaffolds in drug discovery, we herein report a novel NH₄I‑involved oxidative annulation of readily available 2,1‑benzisoxazoles/isatoic anhydrides with benzylic alcohols for the selective synthesis of these heterocycles. In this three‑component transformation, ammonium iodide serves as both an economical nitrogen source and a co‑oxidant, avoiding the use of additional additives. This metal‑ and additive‑free protocol enables precise cleavage of C─O/N─O bonds with simultaneous formation of C─N bonds in a single operation, exhibiting excellent chemoselectivity, atom economy, and broad functional group tolerance. Additionally, the resulting quinazoline and quinazolinone derivatives are efficiently transformed into high‑value analogues of bioactive molecules, underscoring the synthetic utility of the method.</div></div><div>Owing to the structural importance and synthetic value of quinazoline and quinazolinone scaffolds in drug discovery, we herein report a novel NH₄I‑involved oxidative annulation of readily available 2,1‑benzisoxazoles/isatoic anhydrides with benzylic alcohols for the selective synthesis of these heterocycles. In this three‑component transformation, ammonium iodide serves as both an economical nitrogen source and a co‑oxidant, avoiding the use of additional additives. This metal‑ and additive‑free protocol enables precise cleavage of C─O/N─O bonds with simultaneous formation of C─N bonds in a single operation, exhibiting excellent chemoselectivity, atom economy, and broad functional group tolerance. Additionally, the resulting quinazoline and quinazolinone derivatives are efficiently transformed into high‑value analogues of bioactive molecules, underscoring the synthetic utility of the method.</div><div>A novel NH₄I‑mediated oxidative annulation of readily available 2,1‑benzisoxazoles or isatoic anhydrides with benzylic alcohols has been developed under metal‑ and additive‑free conditions, enabling the selective synthesis of quinazoline and quinazolinone derivatives. \u0000<span><figure><span><img><ol><li><span><span>Download: <span>Download high-res image (88KB)</span></span></span></li><li><span><span>Download: <span>Download full-size image</span></span></span></li></ol></span></figure></span></div>","PeriodicalId":130,"journal":{"name":"Asian Journal of Organic Chemistry","volume":"15 8","pages":"Article e70527"},"PeriodicalIF":2.3,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148784285","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis of Tetrasubstituted 2‐Pyrrolines via Zn(II)‐Catalyzed [3+2] Annulation of NH2‐Enaminones and N‐Tosylaziridines","authors":"Qingna Yang,&nbsp;Yan Xie,&nbsp;Liang Xie,&nbsp;Xinying Li,&nbsp;Ziyan Wu,&nbsp;Yucai Jiang,&nbsp;Huiyan Lou,&nbsp;Lulu Chen,&nbsp;Changyuan Zhang","doi":"10.1002/ajoc.70520","DOIUrl":"10.1002/ajoc.70520","url":null,"abstract":"<div><div>A Zn(II)‐catalyzed [3+2] annulation of NH₂‐enaminones with N‐tosylaziridines is described. Various NH₂‐enaminones, along with diversely substituted N‐tosylaziridines, underwent this transformation to deliver tetrasubstituted 2‐pyrrolines in 44%–98% yields under mild conditions. This protocol offers broad substrate scope, good functional group tolerance, and high regioselectivity. Additionally, the resulting tetrasubstituted 2‐pyrrolines could be oxidized to pyrrole (under air/TFA) or undergo tosyl migration (under KOH), highlighting their synthetic versatility.</div></div><div>A Zn(II)‐catalyzed [3+2] annulation of NH₂‐enaminones with N‐tosylaziridines is described. Various NH₂‐enaminones, along with diversely substituted N‐tosylaziridines, underwent this transformation to deliver tetrasubstituted 2‐pyrrolines in 44%–98% yields under mild conditions. This protocol offers broad substrate scope, good functional group tolerance, and high regioselectivity. Additionally, the resulting tetrasubstituted 2‐pyrrolines could be oxidized to pyrrole (under air/TFA) or undergo tosyl migration (under KOH), highlighting their synthetic versatility.</div><div>A Zn(II)‐catalyzed [3+2] annulation of NH₂‐enaminones with N‐tosylaziridines is developed, delivering tetrasubstituted 2‐pyrrolines in 44%–98% yields. This protocol represents a regioselective and versatile approach to tetrasubstituted 2‐pyrrolines, which can be further transformed into pyrroles or undergo tosyl migration, underscoring their synthetic utility.\u0000<span><figure><span><img><ol><li><span><span>Download: <span>Download high-res image (33KB)</span></span></span></li><li><span><span>Download: <span>Download full-size image</span></span></span></li></ol></span></figure></span></div>","PeriodicalId":130,"journal":{"name":"Asian Journal of Organic Chemistry","volume":"15 8","pages":"Article e70520"},"PeriodicalIF":2.3,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148784355","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Silver Carbonate–Enabled Desulfurative Amidation of β‐Acyl Allyl Sulfides for the Construction of Amide‐Substituted α‐Branched Enones","authors":"Qin‐Qin Dang,&nbsp;Hui Li,&nbsp;Qi Zhang,&nbsp;Xu Tian,&nbsp;Zhen‐Kang Wen","doi":"10.1002/ajoc.70529","DOIUrl":"10.1002/ajoc.70529","url":null,"abstract":"<div><div>Herein, we disclose a silver carbonate–mediated approach for desulfurative formation of C─N bonds. The reaction utilizes β‐acyl allylic sulfides in combination with readily available electron‐deficient N–H nucleophiles to access amide‐ and amine‐substituted α‐branched enones. A wide range of N─H nucleophiles is compatible with this transformation, including sulfonamides, phthalimides, as well as diverse (hetero)aromatic and aliphatic amines. Mechanistic studies suggest that the reaction proceeds via initial nucleophilic addition of the N─H nucleophile to the C═C bond of the β‐acyl allylic sulfide, followed by elimination of a methanethiolate anion. Notably, the reaction manifold can be extended beyond C─N bond formation to enable desulfurative C─O and C─C bond construction using N‐protected amino acids and carbon‐based nucleophiles.</div></div><div>Herein, we disclose a silver carbonate–mediated approach for desulfurative formation of C─N bonds. The reaction utilizes β‐acyl allylic sulfides in combination with readily available electron‐deficient N–H nucleophiles to access amide‐ and amine‐substituted α‐branched enones. A wide range of N─H nucleophiles is compatible with this transformation, including sulfonamides, phthalimides, as well as diverse (hetero)aromatic and aliphatic amines. Mechanistic studies suggest that the reaction proceeds via initial nucleophilic addition of the N─H nucleophile to the C═C bond of the β‐acyl allylic sulfide, followed by elimination of a methanethiolate anion. Notably, the reaction manifold can be extended beyond C─N bond formation to enable desulfurative C─O and C─C bond construction using N‐protected amino acids and carbon‐based nucleophiles.</div><div>A silver carbonate‐mediated desulfurative amidation of β‐acyl allylic sulfides with N─H nucleophiles is reported. This method provides efficient access to α‐branched enones across a broad substrate scope including sulfonamides, phthalimides, and amines. Importantly, the methodology is also applicable to desulfurative C─O and C─C bond formation using N‐protected amino acids and carbon nucleophiles.\u0000<span><figure><span><img><ol><li><span><span>Download: <span>Download high-res image (28KB)</span></span></span></li><li><span><span>Download: <span>Download full-size image</span></span></span></li></ol></span></figure></span></div>","PeriodicalId":130,"journal":{"name":"Asian Journal of Organic Chemistry","volume":"15 8","pages":"Article e70529"},"PeriodicalIF":2.3,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148952596","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Elemental Sulfur Mediated Cyclization of Amidoximes and Sulfoxonium Ylides to Access 5‐Acyl‐1,2,4‐Oxadiazoles","authors":"Tien V. Le,&nbsp;Hoang T. Diep,&nbsp;Hoang V. M. Trinh,&nbsp;Vu H. Luu,&nbsp;Tung T. Nguyen","doi":"10.1002/ajoc.70513","DOIUrl":"10.1002/ajoc.70513","url":null,"abstract":"<div><div>We report herein a method for the synthesis of 1,2,4‐oxadiazoles via an annulation of amidoximes and sulfoxonium ylides. Elemental sulfur was utilized to activate the methine carbon in the sulfoxonium ylide, which then acts as an active electrophilic center. A wide range of functionalities, including halogen, ester, and tertiary amine groups, were compatible with the reaction conditions. Products were also obtained from alkyl sulfoxonium ylide starting materials, which overcame the current limitation of available methods.</div></div><div>We report herein a method for the synthesis of 1,2,4‐oxadiazoles via an annulation of amidoximes and sulfoxonium ylides. Elemental sulfur was utilized to activate the methine carbon in the sulfoxonium ylide, which then acts as an active electrophilic center. A wide range of functionalities, including halogen, ester, and tertiary amine groups, were compatible with the reaction conditions. Products were also obtained from alkyl sulfoxonium ylide starting materials, which overcame the current limitation of available methods.</div><div>A method to integrate a methine carbon of a sulfoxonium ylide into a five‐membered ring together with heteroatoms of an amidoxime, thus yielding 5‐acyl‐1,2,4‐oxadiazole derivatives, is developed. The transformation was successful owing to the presence of elemental sulfur, presumably via its reaction with the methine carbon to generate a new electrophilic species. Scope of substrates included the tolerance of a handful of useful functionalities. \u0000<span><figure><span><img><ol><li><span><span>Download: <span>Download high-res image (22KB)</span></span></span></li><li><span><span>Download: <span>Download full-size image</span></span></span></li></ol></span></figure></span></div>","PeriodicalId":130,"journal":{"name":"Asian Journal of Organic Chemistry","volume":"15 8","pages":"Article e70513"},"PeriodicalIF":2.3,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148752631","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Steroids With Insecticidal Activity Against the Larvae of Diaphorina citri Kuwayama From Tinospora sagittata","authors":"Fei Liu,&nbsp;Li‐Ming Zhan,&nbsp;Yang Han,&nbsp;Kai‐Cheng Yang,&nbsp;Jia‐Qi Song,&nbsp;Ting Liu,&nbsp;Li‐Jun Zhang,&nbsp;Hai‐Bing Liao","doi":"10.1002/ajoc.70517","DOIUrl":"10.1002/ajoc.70517","url":null,"abstract":"<div><div>Twelve steroids (<strong>1</strong>−<strong>12</strong>) including one undescribed and a new natural product were isolated from the roots of <em>Tinospora sagittata</em>. The chemical structures of those compounds were elucidated by spectroscopic methods, electronic circular dichroism (ECD) or single‐crystal x‐ray diffraction analysis. Notably, compounds <strong>2</strong> and <strong>3</strong> are a pair of C‐5 epimers. Except for compounds <strong>3</strong> and <strong>4</strong>, the remaining compounds were isolated from <em>Tinospora sagittata</em> (<em>T. sagittata</em>) for the first time. Biologically, at a concentration of 1 and 10 mg/L, two compounds showed insecticide activity. Especially, at a concentration of 10 mg/L, compounds <strong>6</strong> and <strong>12</strong> showed the potent activities, with corrected mortality rates of 68.42% and 71.07%, comparable to that of the positive control spirotetramat (71.07%). Research on the potential insecticidal mechanism of compound <strong>12</strong> revealed that six target proteins were predicted via network pharmacology and molecular docking analyses, with EGFR subsequently identified as the most probable target through western blot verification.</div></div><div>Twelve steroids (<strong>1</strong>−<strong>12</strong>) including one undescribed and a new natural product were isolated from the roots of <em>Tinospora sagittata</em>. The chemical structures of those compounds were elucidated by spectroscopic methods, electronic circular dichroism (ECD) or single‐crystal x‐ray diffraction analysis. Notably, compounds <strong>2</strong> and <strong>3</strong> are a pair of C‐5 epimers. Except for compounds <strong>3</strong> and <strong>4</strong>, the remaining compounds were isolated from <em>Tinospora sagittata</em> (<em>T. sagittata</em>) for the first time. Biologically, at a concentration of 1 and 10 mg/L, two compounds showed insecticide activity. Especially, at a concentration of 10 mg/L, compounds <strong>6</strong> and <strong>12</strong> showed the potent activities, with corrected mortality rates of 68.42% and 71.07%, comparable to that of the positive control spirotetramat (71.07%). Research on the potential insecticidal mechanism of compound <strong>12</strong> revealed that six target proteins were predicted via network pharmacology and molecular docking analyses, with EGFR subsequently identified as the most probable target through western blot verification.</div><div>Twelve steroids including one new compound were isolated and identified from the roots of <em>T. sagittata</em>. This is the first report on the insecticidal activity of steroids to the larvae of <em>Diaphorina citri</em> (<em>D. citri</em>).\u0000<span><figure><span><img><ol><li><span><span>Download: <span>Download high-res image (102KB)</span></span></span></li><li><span><span>Download: <span>Download full-size image</span></span></span></li></ol></span></figure></span></div>","PeriodicalId":130,"journal":{"name":"Asian Journal of Organic Chemistry","volume":"15 8","pages":"Article e70517"},"PeriodicalIF":2.3,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148753675","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Lewis Base‐Catalyzed [3 + 2] Annulation Reaction of 4‐Oxo‐Acrylamides With 2‐Pyrones: Synthesis of Tetrahydropyrano[2,3‐b]Pyrrole‐2,6‐Diones","authors":"Xu‐Na Mao,&nbsp;Rui Yan,&nbsp;Jibing Zhang,&nbsp;Zhaoxue Wang,&nbsp;Ping Wu,&nbsp;Lingang Wu,&nbsp;Jun Li,&nbsp;Lei Xie","doi":"10.1002/ajoc.70532","DOIUrl":"10.1002/ajoc.70532","url":null,"abstract":"<div><div>Herein, an Et₃N‐catalyzed [3 + 2] annulation reaction of 4‐oxo‐acrylamides with 2‐pyrones has been achieved under mild reaction conditions, providing straightforward access to a series of highly functionalized tetrahydropyrano[2,3‐b]pyrrole‐2,6‐dione derivatives in satisfactory results (52%–93% yields with &gt;20:1 drs). In addition, this protocol features transition‐metal‐free conditions, excellent chemoselectivity, and ready applicability to further derivatization.</div></div><div>Herein, an Et₃N‐catalyzed [3 + 2] annulation reaction of 4‐oxo‐acrylamides with 2‐pyrones has been achieved under mild reaction conditions, providing straightforward access to a series of highly functionalized tetrahydropyrano[2,3‐b]pyrrole‐2,6‐dione derivatives in satisfactory results (52%–93% yields with &gt;20:1 drs). In addition, this protocol features transition‐metal‐free conditions, excellent chemoselectivity, and ready applicability to further derivatization.</div><div>A practical Et₃N‐catalyzed annulation reaction between 4‐oxo‐acrylamides and 2‐pyrones has been developed, delivering diverse tetrahydropyrano[2,3‐b]pyrrole‐2,6‐diones in 52%–93% yields with &gt; 20:1 drs. The utility of this transformation is underscored by successful gram‐scale operation and the potential for diverse downstream functionalization, offering a robust platform for accessing complex heterocyclic compounds.\u0000<span><figure><span><img><ol><li><span><span>Download: <span>Download high-res image (24KB)</span></span></span></li><li><span><span>Download: <span>Download full-size image</span></span></span></li></ol></span></figure></span></div>","PeriodicalId":130,"journal":{"name":"Asian Journal of Organic Chemistry","volume":"15 8","pages":"Article e70532"},"PeriodicalIF":2.3,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148952597","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Biochar‐Supported Cu‐MOF as a Highly Efficient Catalyst for the Condensation of L‐Lactic Acid to L‐Lactide","authors":"Meng Ge,&nbsp;Guangshu Yuan,&nbsp;Ruiqi Li,&nbsp;Xu Zhang,&nbsp;Lei Yu","doi":"10.1002/ajoc.70490","DOIUrl":"10.1002/ajoc.70490","url":null,"abstract":"<div><div>Polylactic acid (PLA) is a key biodegradable polymer for green manufacturing. <em>L</em>‐Lactide, the essential intermediate for PLA synthesis, urgently requires efficient and sustainable catalytic production. In this study, a chicken manure‐derived biochar‐supported Cu‐MOF (HKUST‐1@biochar) was fabricated as a novel heterogeneous catalyst for <em>L</em>‐lactic acid condensation to <em>L</em>‐lactide. The biochar support significantly exposed active Cu²⁺ sites and boosted catalytic efficiency. The catalyst afforded <em>L</em>‐lactide with 73.3% yield and 97.8% optical purity, and maintained high activity over five recycling runs. This work achieves waste valorization and green catalysis simultaneously, offering a practical, low‐cost route for industrial <em>L</em>‐lactide production.</div></div><div>Polylactic acid (PLA) is a key biodegradable polymer for green manufacturing. <em>L</em>‐Lactide, the essential intermediate for PLA synthesis, urgently requires efficient and sustainable catalytic production. In this study, a chicken manure‐derived biochar‐supported Cu‐MOF (HKUST‐1@biochar) was fabricated as a novel heterogeneous catalyst for <em>L</em>‐lactic acid condensation to <em>L</em>‐lactide. The biochar support significantly exposed active Cu²⁺ sites and boosted catalytic efficiency. The catalyst afforded <em>L</em>‐lactide with 73.3% yield and 97.8% optical purity, and maintained high activity over five recycling runs. This work achieves waste valorization and green catalysis simultaneously, offering a practical, low‐cost route for industrial <em>L</em>‐lactide production.</div><div>The present work reports a new method for the preparation of biochar and Cu‐MOF composites for the catalytic synthesis of <em>L</em>‐Lactide. The relatively safe and green features of this method make it more suitable for large‐scale application.\u0000<span><figure><span><img><ol><li><span><span>Download: <span>Download high-res image (9KB)</span></span></span></li><li><span><span>Download: <span>Download full-size image</span></span></span></li></ol></span></figure></span></div>","PeriodicalId":130,"journal":{"name":"Asian Journal of Organic Chemistry","volume":"15 8","pages":"Article e70490"},"PeriodicalIF":2.3,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148753039","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Electrocatalytic Synthesis of Dithiosulfonates From Tetrasulfides and Sodium Arylsulfinates","authors":"Xiaoxiao Li,&nbsp;Yingming Song,&nbsp;Yue Yu,&nbsp;Wei Wang","doi":"10.1002/ajoc.70521","DOIUrl":"10.1002/ajoc.70521","url":null,"abstract":"&lt;div&gt;&lt;div&gt;Sustainable unsymmetrical disulfide synthesis is of significant interest due to the crucial role of disulfide bonds in protein stabilization, peptide drug design, and medicinal chemistry, as exemplified by Disulfiram and ADT‐OH. Additionally, sulfone‐containing compounds such as Eletriptan and Dapsone exhibit important pharmaceutical activities. Combining these two motifs, dithiosulfonates (compounds containing a S–S–S(O)&lt;sub&gt;2&lt;/sub&gt; linkage) represent a class of compounds with high research potential. Traditional methods for unsymmetrical disulfide synthesis suffer from malodorous thiols, overoxidation, toxicity, and reliance on precious metals. Although pre‐activation strategies using RSSTs reagents have enabled efficient cross‐coupling, the preparation of RSSTs themselves remains challenging, with conventional routes suffering from low atom economy and toxicity, while photocatalytic approaches require expensive iridium catalysts. Herein, we report a mild, transition‐metal‐free electrochemical approach for the synthesis of dithiosulfonates from tetrasulfides and sodium arylsulfinates. This method avoids malodorous thiols, toxic reagents, and precious metal catalysts, providing a greener and more sustainable route to structurally diverse dithiosulfonates.&lt;/div&gt;&lt;/div&gt;&lt;div&gt;Sustainable unsymmetrical disulfide synthesis is of significant interest due to the crucial role of disulfide bonds in protein stabilization, peptide drug design, and medicinal chemistry, as exemplified by Disulfiram and ADT‐OH. Additionally, sulfone‐containing compounds such as Eletriptan and Dapsone exhibit important pharmaceutical activities. Combining these two motifs, dithiosulfonates (compounds containing a S–S–S(O)&lt;sub&gt;2&lt;/sub&gt; linkage) represent a class of compounds with high research potential. Traditional methods for unsymmetrical disulfide synthesis suffer from malodorous thiols, overoxidation, toxicity, and reliance on precious metals. Although pre‐activation strategies using RSSTs reagents have enabled efficient cross‐coupling, the preparation of RSSTs themselves remains challenging, with conventional routes suffering from low atom economy and toxicity, while photocatalytic approaches require expensive iridium catalysts. Herein, we report a mild, transition‐metal‐free electrochemical approach for the synthesis of dithiosulfonates from tetrasulfides and sodium arylsulfinates. This method avoids malodorous thiols, toxic reagents, and precious metal catalysts, providing a greener and more sustainable route to structurally diverse dithiosulfonates.&lt;/div&gt;&lt;div&gt;An electrochemical strategy for unsymmetrical dithiosulfonate synthesis from tetrasulfides and sodium arylsulfinates is reported, providing a mild, metal‐free approach to RSSTs reagents. This transition‐metal‐free method avoids malodorous thiols, toxic reagents, and precious metal catalysts (e.g., Ir), offering a greener route to S–S–S(O)&lt;sub&gt;2&lt;/sub&gt;‐linked compounds of pharmaceutical relevance.\u0000&lt;span&gt;&lt;figu","PeriodicalId":130,"journal":{"name":"Asian Journal of Organic Chemistry","volume":"15 8","pages":"Article e70521"},"PeriodicalIF":2.3,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148784353","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Photo‐Induced Radical 1,2‐Aminosulfonylation of Alkene to Synthesize β‐Amino Sulfonamides","authors":"Shuai‐Xiao Lu,&nbsp;Yan‐Bing Wei,&nbsp;Wen‐Chao Yang,&nbsp;Yong Zhang","doi":"10.1002/ajoc.70518","DOIUrl":"10.1002/ajoc.70518","url":null,"abstract":"<div><div>Herein, we demonstrate the use of N─N bond cleavage and imine distal migration in photoinduced 1,2‐aminosulfonylation of alkene to synthesize β‐amino sulfonamides. The protocol features room temperature conditions, photocatalyst‐free, transition metal‐free synthesis, high yields, and simple operation.</div></div><div>Herein, we demonstrate the use of N─N bond cleavage and imine distal migration in photoinduced 1,2‐aminosulfonylation of alkene to synthesize β‐amino sulfonamides. The protocol features room temperature conditions, photocatalyst‐free, transition metal‐free synthesis, high yields, and simple operation.</div><div>A domino N─N bond cleavage and imine distal migration in photoinduced 1,2‐aminosulfonylation of alkene was reported to synthesize β‐amino sulfonamides.\u0000<span><figure><span><img><ol><li><span><span>Download: <span>Download high-res image (20KB)</span></span></span></li><li><span><span>Download: <span>Download full-size image</span></span></span></li></ol></span></figure></span></div>","PeriodicalId":130,"journal":{"name":"Asian Journal of Organic Chemistry","volume":"15 8","pages":"Article e70518"},"PeriodicalIF":2.3,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148784354","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Convenient Synthesis of Acrylanilides via K2CO3‐Mediated Deacylative Olefination of Acetoacetanilides","authors":"Subhasis Pal,&nbsp;Rajesh Nandi,&nbsp;Anindya S. Manna,&nbsp;Prakash K. Mandal,&nbsp;Dilip K. Maiti","doi":"10.1002/ajoc.70488","DOIUrl":"10.1002/ajoc.70488","url":null,"abstract":"<div><div>A new and stereoselective E‐olefination strategy has been developed utilizing potassium carbonate (K₂CO₃) as a mild and environmentally benign base. This protocol enables the transformation of β‐ketoamides and aldehydes into the valuable acrylanilides through an acyl bond cleavage. The process involves initial enolate formation, followed by an aldol‐type addition that proceeds through deacetylation to generate the desired C═C bond with elimination of byproduct. This metal‐free, and mild base‐promoted protocol provides a wide substrate scope with stereoselectivity and good to excellent yields, demonstrating a synthetically valuable route for acrylanilides synthesis and thereby for accessing several active pharmaceutical ingredients with potential acceleration in drug discovery efforts, having minimized ecological impact.</div></div>","PeriodicalId":130,"journal":{"name":"Asian Journal of Organic Chemistry","volume":"15 7","pages":"Article e70488"},"PeriodicalIF":2.3,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148466837","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}