Tetrahedron Letters

Amination of aryl halides using copper catalysis

F Lang, D Zewge, IN Houpis, RP Volante

Index: Lang, Fengrui; Zewge, Daniel; Houpis, Ioannis N.; Volante Tetrahedron Letters, 2001 , vol. 42, # 19 p. 3251 - 3254

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Citation Number: 163

Abstract

Bromopyridine 4 was converted into aminopyridine 5 under Cu2O catalysis with an ethylene glycol solution of ammonia in excellent yield (90%). The amination reaction features low (0.5 mol%) catalyst loading, mild reaction temperature (80° C) and low reaction pressure (50 psi). This protocol is further studied in the amination of a variety of aryl halides.