Solid-phase synthesis of functionalized 1,2,4-triazin-6-ones

Published in: Journal, Volume : 43, Issue : 45, Pages : 8165-8167

DOI : 10.1016/s0040-4039(02)01956-1

Author : Blass, Benjamin E.; Coburn, Keith R.; Faulkner, Amy L.; Liu, Song; Ogden, Adam; Portlock, David E.; Srivastava, Anil

Abstract : The solid supported synthesis of functionalized 1,2,4-triazin-6-ones from resin bound amino acids and acid chlorides is described. A thioamide intermediate is generated with Lawesson’s reagent, and the final products are cyclized and cleaved from resin with hydrazine. The products are obtained in good yield and purity.