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Facile Synthesis of Silanols via Cesium Carbonate Catalyzed Hydrosilanes with Water 通过碳酸铯催化水合硅烷轻松合成硅烷醇
Synthesis Pub Date : 2024-09-12 DOI: 10.1055/a-2385-4181
Yunfeng Bai, Miaomiao Chai, Cong Ma, Zhengang Han
{"title":"Facile Synthesis of Silanols via Cesium Carbonate Catalyzed Hydrosilanes with Water","authors":"Yunfeng Bai, Miaomiao Chai, Cong Ma, Zhengang Han","doi":"10.1055/a-2385-4181","DOIUrl":"https://doi.org/10.1055/a-2385-4181","url":null,"abstract":"<p>The demand for green and efficient methods for preparing silanols is significant. In this study, we employed inexpensive cesium carbonate as a catalyst to facilitate the hydrolysis of hydrosilanes for silanol production. This approach offers numerous advantages, including mild reaction conditions, broad substrate compatibility, straightforward post-treatment procedures, high yields, and scalability to gram-level synthesis. Our method demonstrated compatibility with diverse organosilanes bearing alkyl, aryl, alkynyl, and heterocyclic substituents, including sterically hindered variants. The significance of these findings extends beyond scientific inquiry, offering practical utility in the synthesis of silanols.</p> ","PeriodicalId":501298,"journal":{"name":"Synthesis","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207417","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery Process Chemistry: An Innovation Hub at the Interface of Academia, the Pharmaceutical Industry, and Contract Research Organization 发现过程化学：学术界、制药业和合同研究组织之间的创新枢纽
Synthesis Pub Date : 2024-09-11 DOI: 10.1055/a-2380-6425
Matthew A. Horwitz
{"title":"Discovery Process Chemistry: An Innovation Hub at the Interface of Academia, the Pharmaceutical Industry, and Contract Research Organization","authors":"Matthew A. Horwitz","doi":"10.1055/a-2380-6425","DOIUrl":"https://doi.org/10.1055/a-2380-6425","url":null,"abstract":"<p>Discovery Process Chemistry (DPC) is an emerging intersectoral space that is characterized by the development of new chemical reactions or syntheses that enable the efficient elucidation of structure-activity relationships (SARs) and structure-property relationships (SPRs) as well as a rapid transition to process development. Drug discovery and development are accelerated by such efforts and this has led chemists in academia and industry alike to place an increasing importance on these aims. In this Short Review, we explore recent advances in DPC and the impact that it can have on SAR/SPR interrogation and downstream drug development efforts.</p> <p>1 Introduction</p> <p>2 Enabling SAR/SPR Interrogation with Bioisosteres</p> <p>3 Couplings of Diversifiable Reaction Partners</p> <p>4 Late-Stage Functionalization</p> <p>5 Conclusion and Outlook</p> ","PeriodicalId":501298,"journal":{"name":"Synthesis","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207421","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Accessing a Medicinal-Chemistry-Relevant Chemical Space with sp2–sp3 Hybrid Heterocyclic Fragments 利用 sp2-sp3 杂环片段进入药物化学相关的化学空间
Synthesis Pub Date : 2024-09-09 DOI: 10.1055/s-0040-1720137
Raquel Mato, Colin Bournez, Quentin Lefebvre
{"title":"Accessing a Medicinal-Chemistry-Relevant Chemical Space with sp2–sp3 Hybrid Heterocyclic Fragments","authors":"Raquel Mato, Colin Bournez, Quentin Lefebvre","doi":"10.1055/s-0040-1720137","DOIUrl":"https://doi.org/10.1055/s-0040-1720137","url":null,"abstract":"<p>Target-first drug discovery relies heavily on protein structure information, which severely limits its application. In recent years, fragment-based drug Design (FBDD) has been identified as an alternative solution, where screening of smaller molecules for lower affinity allowed the use of focused libraries with a higher hit rate. It is shown that coupling an sp<sup>2</sup>-rich heteroaromatic group with a monofunctional sp<sup>3</sup>-rich core gives fragments (186 examples) with advantageous physical-chemical properties, covering a chemical space often neglected in traditional libraries.</p> ","PeriodicalId":501298,"journal":{"name":"Synthesis","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207418","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Recent Advances in Diazophosphonate Chemistry: Reactions and Transformations 重氮膦酸盐化学的最新进展：反应与转化
Synthesis Pub Date : 2024-09-05 DOI: 10.1055/s-0040-1720129
Saif Ullah, Zulfiqar Hussain, Yungui Peng
{"title":"Recent Advances in Diazophosphonate Chemistry: Reactions and Transformations","authors":"Saif Ullah, Zulfiqar Hussain, Yungui Peng","doi":"10.1055/s-0040-1720129","DOIUrl":"https://doi.org/10.1055/s-0040-1720129","url":null,"abstract":"<p>Diazophosphonates function as indispensable synthetic intermediates within the domain of organic chemistry, serving as precursors for a diverse range of molecules, with potential applications as bioactive compounds. α-Diazomethylphosphonates showcase expansive reactivity and elevated levels of enantioselectivity in asymmetric transformations, especially in conjunction with suitable catalyst systems. This review compiles the latest advancements in diazophosphonate chemistry from 2016 to 2024, highlighting their reactivity and transformative potential in organic synthesis. Diazophosphonates, regarded as revolutionary compounds, exhibit unique attributes as carbene precursors, driving diverse chemical reactions such as [3+2] cycloaddition, asymmetric [3+2] cycloaddition, asymmetric [3+3] cycloaddition, and asymmetric substitution reactions. Their adaptability in functional group conversions underscores their pivotal role in various synthetic methodologies. The review highlights the growing interest in diazophosphonate reactions among synthetic chemists, fostering novel synthetic strategies and expanding their application horizons. The multifaceted utility of diazophosphonates as reagents, synthetic intermediates, precursors, and catalysts underscores their significance in modern organic chemistry and pharmaceutical applications, prompting further exploration into this dynamic field.</p> <p>1 Introduction</p> <p>2 [3+2] Cycloaddition Reactions</p> <p>3 Asymmetric [3+2] Cycloaddition Reactions</p> <p>4 Asymmetric [3+3] Cycloaddition Reactions</p> <p>5 Asymmetric Substitution Reactions</p> <p>6 Diazophosphonates as Carbene Precursors</p> <p>7 Diazophosphonates in the Chemistry of Fluorinated Compounds</p> <p>8 Other Reactions</p> <p>9 Future Directions</p> <p>10 Conclusion</p> ","PeriodicalId":501298,"journal":{"name":"Synthesis","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207419","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Recent Advances in Fluoroalkylation Strategies: Exploring Novel Reactivities and Synthetic Applications of Sulfone- and Sulfinate-Based Reagents for Mono-, Di-, and Trifluoromethylations 氟烷基化策略的最新进展：探索砜基和亚砜基试剂在单、双和三氟甲基化反应中的新型活性和合成应用
Synthesis Pub Date : 2024-09-05 DOI: 10.1055/s-0043-1775391
Alexander Knieb, G. K. Surya Prakash
{"title":"Recent Advances in Fluoroalkylation Strategies: Exploring Novel Reactivities and Synthetic Applications of Sulfone- and Sulfinate-Based Reagents for Mono-, Di-, and Trifluoromethylations","authors":"Alexander Knieb, G. K. Surya Prakash","doi":"10.1055/s-0043-1775391","DOIUrl":"https://doi.org/10.1055/s-0043-1775391","url":null,"abstract":"<p>Fluoroalkylation serves as a pivotal strategy for chemists to precisely alter the properties of small molecules. Among the established fluoroalkylation protocols, sulfone and sulfinate reagents stand out as versatile tools for these reactions, particularly in mono-, di-, and trifluoromethylations. Their versatility lies in offering multiple pathways, encompassing electrophilic, nucleophilic, as well as radical mechanisms, thus providing diverse routes for controlled molecular modifications through a variety of very exciting mechanistic paths.</p> <p>1 Introduction</p> <p>2 Monofluoromethylation Strategies</p> <p>2.1 Fluorobis(phenylsulfonyl)methane (FBSM)</p> <p>2.2 2-Fluoro-1,3-benzodithiole-1,1,3,3-tetraoxide (FBDT)</p> <p>2.3 Benzothiazole-SO<sub>2</sub>CH<sub>2</sub>F, NaSO<sub>2</sub>CH<sub>2</sub>F, and ClSO<sub>2</sub>CH<sub>2</sub>F</p> <p>2.4 PhSO<sub>2</sub>CH<sub>2</sub>F</p> <p>3 Difluoromethylation Strategies</p> <p>3.1 PhSO<sub>2</sub>CF<sub>2</sub>H</p> <p>3.2 Benzothiazole-SO<sub>2</sub>CF<sub>2</sub>H</p> <p>3.3 2-PyrSO<sub>2</sub>CF<sub>2</sub>H</p> <p>3.4 NaSO<sub>2</sub>CF<sub>2</sub>H</p> <p>4 Trifluoromethylation Strategies</p> <p>4.1 PhSO<sub>2</sub>CF<sub>3</sub>\u0000</p> <p>4.2 2-PyrSO<sub>2</sub>CF<sub>3</sub>\u0000</p> <p>4.3 Benzothiazole-SO<sub>2</sub>CF<sub>3</sub>\u0000</p> <p>4.4 NaSO<sub>2</sub>CF<sub>3</sub>\u0000</p> <p>4.4.1 Electrochemical Approaches</p> <p>4.4.2 Photochemical Approaches</p> <p>4.4.3 Other Noteworthy Approaches</p> <p>5 Conclusion</p> ","PeriodicalId":501298,"journal":{"name":"Synthesis","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207420","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Direct Multicomponent Synthesis of C3-Arylated Pyrroles under Catalyst-Free Conditions 在无催化剂条件下直接多组分合成 C3-芳基吡咯
Synthesis Pub Date : 2024-09-04 DOI: 10.1055/a-2380-3855
Amol Prakash Pawar, Reena Jangir, Atul Jankiram Dolas, Yadav Kacharu Nagare, Krishnan Rangan, Eldhose Iype, Indresh Kumar
{"title":"Direct Multicomponent Synthesis of C3-Arylated Pyrroles under Catalyst-Free Conditions","authors":"Amol Prakash Pawar, Reena Jangir, Atul Jankiram Dolas, Yadav Kacharu Nagare, Krishnan Rangan, Eldhose Iype, Indresh Kumar","doi":"10.1055/a-2380-3855","DOIUrl":"https://doi.org/10.1055/a-2380-3855","url":null,"abstract":"<p>An operationally simple catalyst-free protocol for the direct regiospecific synthesis of C3-arylated/alkenylated pyrroles has been developed. The enamine-intermediate, in situ generated from succinaldehyde and a primary amine, was trapped with activated carbonyls before the Paal–Knorr reaction in a direct multicomponent ‘just-mix’ protocol to furnish pyrroles in good yields. Several C3-substituted <i>N</i>-alkylpyrroles have been prepared under open-flask conditions, avoiding protection-deprotection chemistry.</p> ","PeriodicalId":501298,"journal":{"name":"Synthesis","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207422","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of 3-Substituted Chromones through Photoactivation of Acceptor–Acceptor Diazo Compounds 通过光激活受体-受体重氮化合物合成 3-取代的色酮
Synthesis Pub Date : 2024-09-04 DOI: 10.1055/s-0040-1720134
Prashant Kumar, Asit Kumar, Ruchir Kant, Sanjeev K. Shukla, Namrata Rastogi
{"title":"Synthesis of 3-Substituted Chromones through Photoactivation of Acceptor–Acceptor Diazo Compounds","authors":"Prashant Kumar, Asit Kumar, Ruchir Kant, Sanjeev K. Shukla, Namrata Rastogi","doi":"10.1055/s-0040-1720134","DOIUrl":"https://doi.org/10.1055/s-0040-1720134","url":null,"abstract":"<p>We report the photocatalytic alkylation of <i>o</i>-hydroxyarylenaminones with acceptor–acceptor diazo compounds to access 3-alkyl chromones. The reaction involves triplet sensitization of the diazo substrate via energy transfer from the photosensitizer. The notable features of the protocol are operational simplicity, wide substrate scope, and generally high yields of the products.</p> ","PeriodicalId":501298,"journal":{"name":"Synthesis","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142226535","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Electrochemical Trioxygenation of Allylarenes 烯丙基醚的电化学三氧化反应
Synthesis Pub Date : 2024-09-03 DOI: 10.1055/s-0040-1720135
Yong Jiang, Yajuan Li, Chen Zhu, Tao Shen
{"title":"Electrochemical Trioxygenation of Allylarenes","authors":"Yong Jiang, Yajuan Li, Chen Zhu, Tao Shen","doi":"10.1055/s-0040-1720135","DOIUrl":"https://doi.org/10.1055/s-0040-1720135","url":null,"abstract":"<p>Trioxygenation is a highly effective method for rapidly increasing molecular complexity by incorporating three C–O bonds from simple, readily available raw materials. In this study, we present an electrochemical trioxygenation protocol for allylarenes, which enables the synthesis of a diverse array of triacetoxylation products without external chemical oxidants. These products, which are difficult to obtain through conventional methods, highlight the potential of electrochemistry in promoting sustainable synthesis.</p> ","PeriodicalId":501298,"journal":{"name":"Synthesis","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-09-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207423","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of 9,9′-Bifluorenylidene-Based Porous Aromatic Frameworks (BF-PAFs) for Photocatalytic Production of Hydrogen Peroxide 用于光催化生产过氧化氢的 9,9′-双芴基多孔芳香族框架 (BF-PAFs) 的合成
Synthesis Pub Date : 2024-08-28 DOI: 10.1055/a-2378-3919
He Wang, Xinmeng Xu, Linzhu Cao, Xin Tao
{"title":"Synthesis of 9,9′-Bifluorenylidene-Based Porous Aromatic Frameworks (BF-PAFs) for Photocatalytic Production of Hydrogen Peroxide","authors":"He Wang, Xinmeng Xu, Linzhu Cao, Xin Tao","doi":"10.1055/a-2378-3919","DOIUrl":"https://doi.org/10.1055/a-2378-3919","url":null,"abstract":"<p>Photocatalytic technology is considered to be a sustainable strategy to convert H<sub>2</sub>O and O<sub>2</sub> into H<sub>2</sub>O<sub>2</sub>. However, constructing photocatalytically active and stable organic photocatalyst remain a challenge. In this study, a new class of porous aromatic framework photocatalysts (BF-PAFs) were designed and synthesized, in which 9,9′-bifluorenylidene (99′-BF) and different alkynes are alternately connected. The BF-PAFs were constructed and served as photocatalysts for H<sub>2</sub>O<sub>2</sub> synthesis. Experimental results show that the introduction of different alkynes can effectively regulate the optical band gap and energy band structure, which may further determine their photocatalytic performance. Upon visible light irradiation, PAF-370 exhibits high efficiency for photosynthesis of H<sub>2</sub>O<sub>2</sub> with a production rate of 730 μmol g<sup>–1</sup> h<sup>–1</sup> in the presence of sacrificial reagent from water and oxygen via oxygen reduction reaction (ORR) pathway. Furthermore, up to 61 μmol H<sub>2</sub>O<sub>2</sub> could be generated from this photocatalytic system after 14 hours.</p> ","PeriodicalId":501298,"journal":{"name":"Synthesis","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207425","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Photoredox-Catalyzed Synthesis of N-Aryl γ-Lactams via Radical Addition–Cyclization Cascade 光氧化催化下通过自由基加成-环化级联合成 N-芳基 γ-内酰胺
Synthesis Pub Date : 2024-08-28 DOI: 10.1055/a-2378-8663
Aznur Azim, Vidhul Vasudevan, Tanumoy Mandal, Suman De Sarkar
{"title":"Photoredox-Catalyzed Synthesis of N-Aryl γ-Lactams via Radical Addition–Cyclization Cascade","authors":"Aznur Azim, Vidhul Vasudevan, Tanumoy Mandal, Suman De Sarkar","doi":"10.1055/a-2378-8663","DOIUrl":"https://doi.org/10.1055/a-2378-8663","url":null,"abstract":"<p>A visible-light mediated one-pot synthesis of <i>N</i>-aryl γ-lactams is developed following a cascade radical addition/cyclization sequence. This transition metal-free approach proceeds efficiently at room temperature, employing an organic dye as the photocatalyst. Inexpensive <i>N</i>-arylglycines and acrylic acid derivatives were used as the starting materials and a vast array of diversely substituted <i>N</i>-aryl γ-lactams were synthesized in moderate to excellent yields. Detailed mechanistic experiments and comprehensive photophysical studies elucidated a plausible reaction mechanism.</p> ","PeriodicalId":501298,"journal":{"name":"Synthesis","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207426","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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