Palladium catalyzed cross-coupling of 3-methylthiophene-2-carbonyl chloride with aryl/het-aryl boronic acids: a convenient method for synthesis of thienyl ketones

Abstract

Bi-aryl ketones are important motifs in large number of pharmaceutical compounds and natural products. A protocol for the synthesis of thienyl ketones has been developed via Pd (0) catalyzed cross-coupling reaction. The desired thienyl ketones (3a-x) were synthesized by cross coupling of 3-methylthiophene-2-carbonyl chloride with variety of aryl/heteroaryl-boronic acids in good to excellent yields (46–91%) under mild conditions (1.5 eq Cs<inf>2</inf>CO<inf>3</inf> at 50 °C). Different functional groups were well tolerated under the developed reaction conditions. © 2024 Elsevier B.V., All rights reserved.