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A Novel PIFA/KOH Promoted Approach to Synthesize C2-arylacylated Benzothiazoles as Potential Drug Scaffolds.

Authors :
Sun XT
Hu ZG
Huang Z
Zhou LL
Weng JQ
Source :
Molecules (Basel, Switzerland) [Molecules] 2022 Jan 22; Vol. 27 (3). Date of Electronic Publication: 2022 Jan 22.
Publication Year :
2022

Abstract

To discover an efficient and convenient method to synthesize C2-arylacylated benzothiazoles as potential drug scaffolds, a novel [bis(trifluoroacetoxy)iodo]benzene(PIFA)/KOH synergistically promoted direct ring-opening C2-arylacylation reaction of 2H -benzothiazoles with aryl methyl ketones has been developed. Various substrates were tolerated under optimized conditions affording the C2-arylacylation products in 70-95% yields for 38 examples. A plausible mechanism was also proposed based on a series of controlled experiments.

Details

Language :
English
ISSN :
1420-3049
Volume :
27
Issue :
3
Database :
MEDLINE
Journal :
Molecules (Basel, Switzerland)
Publication Type :
Academic Journal
Accession number :
35163992
Full Text :
https://doi.org/10.3390/molecules27030726