通过配体促进的氮杂-Heck环化反应以及N-（五氟苯甲酰氧基）氨基甲酸酯的串联反应合成吡咯烷和哌啶
Pyrrolidines and Piperidines by Ligand-Enabled Aza-Heck Cyclizations and Cascades of N-(Pentafluorobenzoyloxy)carbamates.
作者信息
Hazelden Ian R, Carmona Rafaela C, Langer Thomas, Pringle Paul G, Bower John F
机构信息
School of Chemistry, University of Bristol, Bristol, BS8 1TS, UK.
Pharmaceutical Technology & Development, AstraZeneca, Charter Way, Macclesfield, SK10 2NA, UK.
出版信息
Angew Chem Int Ed Engl. 2018 Apr 23;57(18):5124-5128. doi: 10.1002/anie.201801109. Epub 2018 Mar 22.
Abstract
Ligand-enabled aza-Heck cyclizations and cascades of N-(pentafluorobenzoyloxy)carbamates are described. These studies encompass the first examples of efficient non-biased 6-exo aza-Heck cyclizations. The methodology provides direct and flexible access to carbamate protected pyrrolidines and piperidines.
摘要
描述了配体促进的氮杂-Heck环化反应以及N-(五氟苯甲酰氧基)氨基甲酸酯的串联反应。这些研究包含了高效无偏向的6-外向氮杂-Heck环化反应的首例。该方法为氨基甲酸酯保护的吡咯烷和哌啶提供了直接且灵活的合成途径。
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