Diastereoselective synthesis of 3-substituted acylamino-3,4-dihydro-1,2,4-triazinones

Abstract

6-Phenyl-1,2,4-triazin-5(4H)-one 1 reacts with C-nucleophiles, such as indole, in the presence of N-acetylamino acids, to yield 2-acyl-3-indolyl-6-phenyl-3,4-dihydro-1,2,4-triazin-5(4H)-ones 2-6 with high diastereoselectivity.