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Iron‐catalyzed C(5)−H Imidation of Azole with N ‐Fluorobenzenesulfonimide
Author(s) -
Wang Xiaojiao,
Lei Bowen,
Ma Lifang,
Jiao Huixuan,
Xing Wenhua,
Chen Jiaming,
Li Ziyuan
Publication year - 2017
Publication title -
advanced synthesis and catalysis
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.541
H-Index - 155
eISSN - 1615-4169
pISSN - 1615-4150
DOI - 10.1002/adsc.201701124
Subject(s) - chemistry , oxazole , reagent , azole , thiazole , combinatorial chemistry , medicinal chemistry , stereochemistry , organic chemistry , antifungal , medicine , dermatology
An iron(II)‐catalyzed direct imidation of oxazole and thiazole with N ‐fluorobenzenesulfonimide (NFSI) through C(5)−H bond cleavage is disclosed, providing C5‐imidated azoles in moderate to excellent yields with broad substrate scope. This reaction represents the first iron‐catalyzed C−H imidation of arene where NFSI serves as the imidation reagent, and potentially constitutes an efficient access to C5‐functionalized azole with great medicinal significance.

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