Abstract

A new user-friendly and convenient method for the acetylation of N-heteroaryl bromides is described. This process is based on the palladium-catalyzed olefination of an N-heteroaryl bromide with butyl vinyl ether, followed by acid hydrolysis of the intermediate heteroaryl vinyl ether in situ. Isopropanol at 85 °C, in the presence of K 3 PO 4 ·3H 2 O (2 equiv), PdCl 2 (2 mol%) and ( O-tolyl) 3 P (4 mol%), provided the best conditions, giving yields of N-heteroaryl bromides up to 75%.

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