Efficient and regioselective one-step synthesis of 7-aryl-5-methyl- and 5-aryl-7-methyl-2-amino-[1,2,4]triazolo[1,5-a]pyrimidine derivatives
作者:Serena Massari、Jenny Desantis、Giulio Nannetti、Stefano Sabatini、Sara Tortorella、Laura Goracci、Violetta Cecchetti、Arianna Loregian、Oriana Tabarrini
DOI:10.1039/c7ob02085f
日期:——
facile and efficient one-step procedures for the regioselective synthesis of 7-aryl-5-methyl- and 5-aryl-7-methyl-2-amino-[1,2,4]triazolo[1,5-a]pyrimidines have been developed, via reactions of 3,5-diamino-1,2,4-triazole with variously substituted 1-aryl-1,3-butanediones and 1-aryl-2-buten-1-ones, respectively. The excellent yield and/or regioselectivity shown by the reactions decreased when ethyl 5-amino-1
区域选择性合成7-芳基-5-甲基-和5-芳基-7-甲基-2-氨基-[1,2,4]三唑并[1,5-a]嘧啶的两种简便有效的一步步骤通过3,5-二氨基-1,2,4-三唑分别与各种取代的1-芳基-1,3-丁二酮和1-芳基-2-丁烯-1-酮的反应,已经开发出。当使用5-氨基-1,2,4-三唑-3-羧酸乙酯时,反应显示的优异的产率和/或区域选择性降低。作为[1,2,4]三唑并[1,5-a]嘧啶的特有支架,本文报道的方法可用于制备生物活性化合物。在这项研究中,基于[1,2,4] triazolo [1,