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Advanced Synthesis & Catalysis最新文献

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Stereoselective Palladium-Catalyzed C(sp3)–H Mono-Arylation of Piperidines and Tetrahydropyrans with a C(4) Directing Group 带C(4)导向基团的胡椒啶和四氢吡喃的立体选择性钯催化C(sp3) -H单芳基化
Advanced Synthesis & Catalysis Pub Date : 2021-11-08 DOI: 10.33774/chemrxiv-2021-ks58d
Amalia-Sofia Piticari, Daniele Antermite, Joe I Higham, J. Moore, Matthew P. Webster, J. Bull
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引用次数: 4
Synthesis of α- and β-Carbolines by a Metalation/Negishi Cross-Coupling/SNAr Reaction Sequence 金属化/根岸交叉偶联/SNAr反应序列合成α-和β-碳胺
Advanced Synthesis & Catalysis Pub Date : 2021-08-26 DOI: 10.33774/CHEMRXIV-2021-P8WCV
Shainthavaan Sathiyalingam, Stefan Roesner
{"title":"Synthesis of α- and β-Carbolines by a Metalation/Negishi Cross-Coupling/SNAr Reaction Sequence","authors":"Shainthavaan Sathiyalingam, Stefan Roesner","doi":"10.33774/CHEMRXIV-2021-P8WCV","DOIUrl":"https://doi.org/10.33774/CHEMRXIV-2021-P8WCV","url":null,"abstract":"Carbolines are considered to be privileged scaffolds in medicinal chemistry. An efficient method for the synthesis of α- and β-carbolines from fluoropyridines and 2-haloanilines is reported. This streamlined procedure consists of a four-step directed ortho-lithiation, zincation, Negishi cross-coupling, and intramolecular nucleophilic aromatic substitution, providing access to a diverse set of functionalized carbolines. While the procedure is applicable to batch conditions, the generation of arylzinc intermediates in continuous flow has been demonstrated.","PeriodicalId":7248,"journal":{"name":"Advanced Synthesis & Catalysis","volume":"44 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-08-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75835543","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: 3
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