Asymmetric Synthesisof Cis -(S , R )-3-Amino-4-Fluoro-1-Methylpyrrolidine

Zhongbo Fei,Xin Xiong, Chiming Cheung,Weipeng Liu,Qirong Shen,Jinzhu Zhang,Hongjun Gao,Jianwei Bian

SYNLETT（2019）

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摘要

The development of the stereoselective synthesis of cis -( S , R )-3-amino-4-fluoro-1-methylpyrrolidine is described starting from chiral, non-racemic 1-[(3 S ,4 S )-3-azido-4-hydroxypyrrolidin-1-yl]-2,2,2-trifluoroethan-1-one. Two sets of deoxyfluorination conditions are developed for achieving inversion of the chiral center with high or complete stereoselectivity.

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关键词

stereoselective, azides, deoxyfluorination, sulfuryl fluoride, pyrrolidines

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