Transition metal-free regioselective direct acylation of quinazolines for the synthesis of acylquinazoline derivatives

Abstract

An efficient method for direct regioselective acylation of quinazolines under metal-free conditions was developed. The acylation reaction of quinazolines gave corresponding acyl quinazolines in ethyl acetate with good to excellent yields and excellent functional group tolerance and site selectivity.

Metal-free, direct acylation of purines to access C6-acylated purine derivatives induced by TBHP via Minisci-type reaction

“…27 For example, recently, Peng et al reported direct acylation of quinazolines in the presence of PhI(OCOCF 3 ) 2 and TMSN 3 without any transition metal catalyst. 28 Encouraged by these developments and our persistent studies on the modification of purines, 29 we tried to develop a green, metal-free, light-free radical reaction to synthesize C 6 -acylated purines via Minisci-type reaction (Scheme 1F).…”