Direct Catalytic Symmetrical, Unsymmetrical N,N-Dialkylation and Cyclization of Acylhydrazides Using Alcohols
作者:Subramanian Thiyagarajan、Chidambaram Gunanathan
DOI:10.1021/acs.orglett.0c02369
日期:2020.8.21
Herein, direct N,N-dialkylation of acylhydrazides using alcohols is reported. This catalytic protocol provides one-pot synthesis of both symmetrical and unsymmetrical N,N-disubstituted acylhydrazides using an assortment of primary and secondary alcohols with remarkable selectivity and excellent yields. Interestingly, the use of diols resulted in intermolecular cyclization of acylhydrazides, and such
在本文中,报道了使用醇将酰肼直接进行N,N-二烷基化。该催化方案使用各种伯醇和仲醇,具有显着的选择性和优异的收率,可以一锅法合成对称和不对称的N,N-二取代的酰肼。有趣的是,使用二醇导致酰肼的分子间环化,并且此类产物是生物活性化合物中的优先结构。水是唯一的副产物,这使得该催化方案可持续且对环境无害。