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Recent Developments in C−H Functionalisation of Benzofurans and Benzothiophenes
Author(s) -
Morgan David,
Yarwood Stephen J.,
Barker Graeme
Publication year - 2021
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.202001470
Subject(s) - benzothiophene , benzofuran , chemistry , indole test , bicyclic molecule , heteroatom , combinatorial chemistry , organic chemistry , ring (chemistry) , thiophene
Benzofurans and benzothiophenes are important pharmaceutical motifs, appearing in a broad range of small molecule therapeutic classes. Often overlooked by synthetic methodologists in favour reactions of the analogous indole bicyclic system, there is nevertheless a plurality of approaches to effecting benzofuran and benzothiophene C−H functionalisations. In this review, we summarise progress in this area over the past five years, including 1) alkylations, 2) arylations and heteroarylations, 3) carboxylations, carbamoylations, and C‐heteroatom bond formations and 4) cyclisations.