Optimized synthesis of tetrahydroisoquinoline-hydantoins

…, AC Gassiot, P Melnyk, S Girault-Mizzi, C Sergheraert

Index: Charton, Julie; Gassiot, Amaury Cazenave; Melnyk, Patricia; Girault-Mizzi, Sophie; Sergheraert, Christian Tetrahedron Letters, 2004 , vol. 45, # 38 p. 7081 - 7085

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Citation Number: 14

Abstract

Several methods have been developed and compared for the solution synthesis of tetrahydroisoquinoline-hydantoin (Tic-hydantoin) derivatives. Starting materials were Tic-OH and amines readily available from commercial sources. The best yields were observed when the imidazolidine-2, 4-dione ring was synthesized in two steps:(1) reaction of Tic-OH with the appropriate amine and (2) cyclization with 1, 1′-carbonyldiimidazole.