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Fluorocyclization of Vinyl Azides for the Formation of 3‐Azido Heterocycles
Author(s) -
Bai Diangang,
Li Linxuan,
Li Xiaomeng,
Lu Ying,
Wu Yong,
Rajendra Prasad Reddy Bhoomireddy,
Ning Yongquan
Publication year - 2020
Publication title -
chemistry – an asian journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.18
H-Index - 106
eISSN - 1861-471X
pISSN - 1861-4728
DOI - 10.1002/asia.202001175
Subject(s) - regioselectivity , combinatorial chemistry , chemistry , azide , functional group , organic chemistry , catalysis , polymer
3‐Azido saturated heterocycles are important for therapeutic‐development but challenging to prepare. Disclosed herein is a novel synthetic strategy for 3‐azido heterocycles via fluorocyclization of the easily available vinyl azides. This transfor‐mation proceeded under mild conditions and provided a wide range of 3‐azido heterocycles in good to excellent yields. Notably, the azido group plays an indispensable role to promote rapid and regioselective fluorocyclization. Moreover, the protocol was highlighted by gram‐scale synthesis and further synthetic transformations.