Recent Developments in C−H Functionalisation of Benzofurans and Benzothiophenes. Issue 7 (22nd December 2020)

• Record Type: Journal Article
• Authors: Morgan, David; Yarwood, Stephen J.; Barker, Graeme
• Is Part Of: European journal of organic chemistry. Issue 7(2021)
• Page Start: 1072
• Page End: 1102
• Publication Date: 2020-12-22
• Subjects: Benzofuran -- Benzothiophene -- Functionalization -- Heterocycles -- Synthetic methods; Chemistry, Organic -- Periodicals; Organic compounds -- Synthesis -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1002/ejoc.202001470
• Languages: English
• ISSNs: 1434-193X

Abstract

Abstract: 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. Abstract : In this review, we summarise progress in benzofuran and benzothiophene C−H functionalisations over the past five years, including 1) alkylations, 2) arylations and heteroarylations, 3) carboxylations, carbamoylations and C‐heteroatom bond formations and 4) cyclisations.