Parusharamudu K (Investigation Methodology) , Bhanu Prasad Banda (Investigation Methodology) , Krishnaiah Atmakur (Conceptualization Methodology Supervision Validation Writing – original draft)
{"title":"A catalyst and solvent free synthesis of polysubstituted 2-methylene-1,2-dihydropyridines","authors":"Parusharamudu K (Investigation Methodology) , Bhanu Prasad Banda (Investigation Methodology) , Krishnaiah Atmakur (Conceptualization Methodology Supervision Validation Writing – original draft)","doi":"10.1080/00397911.2025.2495139","DOIUrl":"10.1080/00397911.2025.2495139","url":null,"abstract":"<div><div>Synthesis of polysubstituted 2-methylene-1,2-dihydropyridines were accomplished by one-pot multicomponent reaction of 3-formylchromones, anilines and aliphatic 1,3-diones under catalyst and solvent-free reaction conditions. The reaction proceeds <em>via</em> Schiff base mediated, Michael addition followed by ring opening/ring closure sequential process resulting two new C–N and one C–C bonds formation. Neat reaction conditions and higher yields are the advantages of the protocol.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 9","pages":"Pages 683-691"},"PeriodicalIF":1.8,"publicationDate":"2025-05-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143929189","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Guojie Yin (Investigation Writing – original draft) , Canli Zhang (Investigation) , Qiong Liu (Data curation Writing – review & editing) , Youju Shu (Data curation) , Weijun Fu (Conceptualization Supervision Writing – original draft)
{"title":"Electrochemical oxidative monofluoromethylation of N-acryl-2-aryl benzimidazoles: access to CFH2-containing benzimidazo[2,1-a]isoquinolin-6(5H)-one derivatives","authors":"Guojie Yin (Investigation Writing – original draft) , Canli Zhang (Investigation) , Qiong Liu (Data curation Writing – review & editing) , Youju Shu (Data curation) , Weijun Fu (Conceptualization Supervision Writing – original draft)","doi":"10.1080/00397911.2025.2493953","DOIUrl":"10.1080/00397911.2025.2493953","url":null,"abstract":"<div><div>An efficient monofluoromethylation of N-acryl-2-aryl benzimidazoles was developed through an electro-oxidative CFH<sub>2</sub>-radical generation, followed by cascade cyclization fabricating a benzimidazo[2,1-a]isoquinolin-6(5H)-one scaffold. The protocol used the readily available CFH<sub>2</sub>SO<sub>2</sub>Na as the monofluoromethylation reagent, enabling the step economical synthesis of polycyclic benzimidazoles in moderate to high yields under metal- and oxidant-free conditions. Furthermore, the reaction mechanism was subjected to investigation, and it was demonstrated that the necessity of anodic oxidation in the cascade process.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 9","pages":"Pages 661-671"},"PeriodicalIF":1.8,"publicationDate":"2025-05-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143929188","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Sweeti (Conceptualization Formal analysis Investigation Methodology Validation Writing – original draft) , Prince Malik (Formal analysis Methodology) , Gyanesh Kumar Mishra (Formal analysis Methodology) , Hemant Nagpal (Formal analysis) , Ajeet Kumar (Formal analysis Resources Supervision) , Ajay Kumar Purohit (Methodology Resources Supervision Writing – original draft) , Mohammed Mohsin (Conceptualization Data curation Investigation Methodology Supervision Writing – original draft Writing – review & editing)
{"title":"Highly effective, rapid and convenient one-pot synthesis of O,O’-dialkyl-N,N-dialkylphosphoramidates from trialkyl phosphites","authors":"Sweeti (Conceptualization Formal analysis Investigation Methodology Validation Writing – original draft) , Prince Malik (Formal analysis Methodology) , Gyanesh Kumar Mishra (Formal analysis Methodology) , Hemant Nagpal (Formal analysis) , Ajeet Kumar (Formal analysis Resources Supervision) , Ajay Kumar Purohit (Methodology Resources Supervision Writing – original draft) , Mohammed Mohsin (Conceptualization Data curation Investigation Methodology Supervision Writing – original draft Writing – review & editing)","doi":"10.1080/00397911.2025.2494244","DOIUrl":"10.1080/00397911.2025.2494244","url":null,"abstract":"<div><div>Verification of Chemical Weapon Convention (CWC) related chemicals necessitates proper synthesis of reference chemicals for their unambiguous identification during off-site analysis. <em>O,O’-</em>dialkyl-<em>N,N</em>-dialkylphosphoramidates are listed in Annex 2.B.6 of CWC as precursor of highly toxic nerve agent ‘Tabun’ (Schedule 1.A.2). Existing methods for synthesis of <em>O,O’-</em>dialkyl-<em>N,N</em>-dialkylphosphoramidates (DADAP’s) rely on utilization of hazardous chlorinating agents in the intermediate stage for chlorination purposes. Herein, we report novel one-pot synthesis of CWC related <em>O,O’-</em>dialkyl-<em>N,N</em>-dialkylphosphoramidates from trialkylphosphites by using iodine and appropriate secondary amines as per convention requirement. Reaction was performed in hexane using iodine as a catalyst. Both hexane and iodine were relatively safe, inexpensive and easy to handle. The developed method was tolerated for the synthesis of various <em>O,O’</em>-dialkyl-<em>N,N</em>-dialkylphosphoramidates (1a–1y). Optimized method gives 88–96% product yield within 15 min at 25 °C. All products were characterized by GC-MS, LC-MS,<sup>1</sup>H NMR and <sup>31</sup>P{<sup>1</sup>H} NMR techniques.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 9","pages":"Pages 672-682"},"PeriodicalIF":1.8,"publicationDate":"2025-05-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143929190","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Preparation of 2-(N-aroylamino)benzothiazoles via intramolecular C-S cyclization approach","authors":"Ratna Babu Gunturu (Investigation Methodology) , Prasanna Babu Racheeti (Investigation Methodology) , Usharani Mandapati (Formal analysis Methodology) , Ramana Tamminana (Supervision Writing – original draft Writing – review & editing) , Rameshraju Rudraraju (Supervision Writing – review & editing)","doi":"10.1080/00397911.2025.2496696","DOIUrl":"10.1080/00397911.2025.2496696","url":null,"abstract":"<div><div>The iron-catalyzed <em>C-S</em> cyclization of variety functional <em>N</em>-2-iodophenyl-N<sup>1</sup>-benzoyl thioureas is successfully carried out to provide 2-(<em>N</em>-aroylamino) benzothiazoles in good to high yield under moderate conditions. Substrate scope tolerance has also been extended. Control experiments confirmed that the reaction mechanism proceeds through intra molecular <em>C-S</em> cross coupling reaction.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 10","pages":"Pages 717-726"},"PeriodicalIF":1.8,"publicationDate":"2025-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143948414","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M Indhupriya (Data curation) , Reddi Mohan Naidu Kalla (Conceptualization) , Sowjanya Bandlapalli (Formal analysis) , Venkata Narayana Palakollu (Validation) , Jaewoong Lee (Supervision)
{"title":"Efficient, neat method for the synthesis of pyrazolyl phosphonates by di-n-butylamine","authors":"M Indhupriya (Data curation) , Reddi Mohan Naidu Kalla (Conceptualization) , Sowjanya Bandlapalli (Formal analysis) , Venkata Narayana Palakollu (Validation) , Jaewoong Lee (Supervision)","doi":"10.1080/00397911.2025.2498532","DOIUrl":"10.1080/00397911.2025.2498532","url":null,"abstract":"<div><div>A three-component, di-<em>n</em>-butylamine-catalyzed, one-pot synthesis of pyrazolyl phosphonates has been developed. Enolizable C–H activated compounds and diethylphosphite were employed to condense a variety of substrates, including various substituted aromatic, fused, and heterocyclic aromatic aldehydes, in order to produce the necessary products in high yields. This technique offers a quick and environmentally benign way to create a diversity-focused pyrazolyl phosphonates. The primary benefits of this approach are its high yields, excellent atom economy (It utilizes the starting materials effectively, minimizing waste and improving sustainability), environmental friendliness, and the fact that it does not require column chromatographic purification for product isolation. Consequently, it provides an alternative method for generating a range of pyrazolylphosphonates within minutes.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 10","pages":"Pages 749-757"},"PeriodicalIF":1.8,"publicationDate":"2025-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143948409","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Xiaobo Zhao (Funding acquisition Writing – original draft) , Zixuan Cha (Investigation) , Xinyue Liu (Investigation) , Jiaqin Liu (Investigation) , Yuheng Zhang (Investigation) , Haifeng Yu (Funding acquisition Project administration Writing – review & editing)
{"title":"Tandem [4C + 2C] cyclization reaction of α-acetyl-α-oxo ketene dithioacetals and acrylonitrile: A straightforward synthesis of polysubstituted cyclohex-3-enones","authors":"Xiaobo Zhao (Funding acquisition Writing – original draft) , Zixuan Cha (Investigation) , Xinyue Liu (Investigation) , Jiaqin Liu (Investigation) , Yuheng Zhang (Investigation) , Haifeng Yu (Funding acquisition Project administration Writing – review & editing)","doi":"10.1080/00397911.2025.2496972","DOIUrl":"10.1080/00397911.2025.2496972","url":null,"abstract":"<div><div>In the investigation, the tandem (Michael addition/nucleophilic cyclization/Michael addition reactions) [4C + 2C] cyclization reaction of α-acetyl-α-oxo ketene dithioacetals as four-carbon synthons and acrylonitrile as two-carbon components is developed under mild reaction conditions. In the presence of 1 equivalents of t-BuOK, the tandem [4C + 2C] cyclization reaction of α-acetyl-α-oxo ketene dithioacetals and acrylonitrile efficiently occur to polysubstituted cyclohex-3-enones in 60–72% yields. Twenty-four new products were synthesized and characterized by NMR, FTIR, HRMS and X-ray crystallography. The approach exhibits fascinating features such less expensive, efficient and operationally convenient, ease of scale-up.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 10","pages":"Pages 727-738"},"PeriodicalIF":1.8,"publicationDate":"2025-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143948412","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Reaction of ethyl 2-(arylidene)acetoacetates, 3-methyl-1H-pyrazol-5(4H)-one, and ammonium acetate: Unexpected formation of bis(pyrazolyl)methanes versus fused pyrazolo-1,4-dihydropyridines","authors":"Adeleh Moshtaghi Zonouz (Supervision) , Nojaba Forghani (Methodology) , Mostafa Razban (Investigation)","doi":"10.1080/00397911.2025.2475908","DOIUrl":"10.1080/00397911.2025.2475908","url":null,"abstract":"<div><div>The reaction of 3-methyl-1<em>H</em>-pyrazol-5(4<em>H</em>)-one, ethyl 2-(arylidene)acetoacetates, and ammonium acetate in refluxing ethanol leads to the formation of 4,4′-(arylmethylene)bis(3-methyl-1<em>H</em>-pyrazolyl-5-ol) derivatives with high yields, instead of the expected fused pyrazolo-1,4-dihydropyridines. This suggests the presence of a reactive vinylogous imino derivative as an intermediate.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 8","pages":"Pages 586-595"},"PeriodicalIF":1.8,"publicationDate":"2025-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144106343","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Xiaojie Hu , Yue Wang , Jicun Wang , Lu Zheng , Qingkun Wu
{"title":"Research progress on synthesis of SGLT-2 inhibitor ertugliflozin","authors":"Xiaojie Hu , Yue Wang , Jicun Wang , Lu Zheng , Qingkun Wu","doi":"10.1080/00397911.2025.2452291","DOIUrl":"10.1080/00397911.2025.2452291","url":null,"abstract":"<div><div>Ertugliflozin, an orally administered sodium-glucose cotransporter 2 (SGLT-2) inhibitor, serves as a therapeutic option for adult patients with diabetes mellitus. This comprehensive review outlines six synthetic routes of Ertugliflozin as documented in the literature, offering a concise analysis of each route to serve as a valuable resource for future synthesis process optimization.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 8","pages":"Pages 577-585"},"PeriodicalIF":1.8,"publicationDate":"2025-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144105346","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"1,2-Aminoalkylacylation of styrenes by cooperative NHC/photoredox dual catalysis","authors":"Lili Wu (Formal analysis Investigation Methodology Writing – original draft) , Chengming Wang (Conceptualization Funding acquisition Project administration Supervision Writing – review & editing)","doi":"10.1080/00397911.2025.2486106","DOIUrl":"10.1080/00397911.2025.2486106","url":null,"abstract":"<div><div>A novel visible-light-mediated 1,2-aminoalkylacylation reaction of styrenes with α-silyl-protected tertiary amines and acyl fluorides has been developed for the efficient construction of γ-aminoketones. This transformation employs a synergistic dual catalyst system, combining the benefits of N-heterocyclic carbene catalysis and photoredox catalysis, enabling the reaction to proceed under mild conditions.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 8","pages":"Pages 618-626"},"PeriodicalIF":1.8,"publicationDate":"2025-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144106344","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pritesh P. Khobrekar (Conceptualization Data curation Formal analysis Methodology Writing – original draft Writing – review & editing) , Pooja V. Shreechippa (Formal analysis) , Rutika R. Gawas (Formal analysis) , Ratan W. Jadhav (Formal analysis) , Vishnu R. Chari (Software) , Sheshanath V. Bhosale (Conceptualization Project administration Supervision Writing – review & editing) , Sandesh T. Bugde (Conceptualization Investigation Project administration Supervision Validation Writing – review & editing)
{"title":"Visible-light-induced aerobic C-3 thiocyanation of indoles using porphyrin as photoredox catalyst","authors":"Pritesh P. Khobrekar (Conceptualization Data curation Formal analysis Methodology Writing – original draft Writing – review & editing) , Pooja V. Shreechippa (Formal analysis) , Rutika R. Gawas (Formal analysis) , Ratan W. Jadhav (Formal analysis) , Vishnu R. Chari (Software) , Sheshanath V. Bhosale (Conceptualization Project administration Supervision Writing – review & editing) , Sandesh T. Bugde (Conceptualization Investigation Project administration Supervision Validation Writing – review & editing)","doi":"10.1080/00397911.2025.2477650","DOIUrl":"10.1080/00397911.2025.2477650","url":null,"abstract":"<div><div>In this work, we report a metal-free and environmentally friendly approach for the electrophilic C–H thiocyanation of indoles under visible light irradiation. Using porphyrin as a photocatalyst and atmospheric air as an oxidant, we developed a mild and efficient route to synthesize a series of thiocyanate products with both electron-rich and electron-deficient systems in moderate to good yields. The use of a radical scavenger like TEMPO helped to establish a photoredox mechanism. This method offers a sustainable and promising approach for synthesizing heterocyclic substrates, thiocyanate aromatics, and bioactive molecules through photoredox catalysis.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 8","pages":"Pages 596-607"},"PeriodicalIF":1.8,"publicationDate":"2025-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144106399","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}