One-Step Construction of 2-Methylquinazolin-4(3H)-ones Using Solid Calcium Carbide as an Alternative to Gaseous Acetylene

作者：Botao Wang, Zhiqiang Wang, Xinjie You, Zheng Li, Jinhui Yang · 发表于：The Journal of Organic Chemistry · 年份：2024 · DOI：10.1021/acs.joc.4c02341 · 被引用次数：15 · 研究领域：Quinazolinone synthesis and applications、Synthesis and bioactivity of alkaloids、Multicomponent Synthesis of Heterocycles

2-Methylquinazolin-4(3 H )-ones were efficiently constructed using solid calcium carbide as an alkyne source, 2-aminobenzamides or 2-aminobenzohydrazides as substrates, and p -tolylsulfonyl azide as a mediator through simultaneous formation of two C–N bonds in one step. The salient features of this protocol are the use of an inexpensive, abundant and easy-to-use alkyne source as a substitute for flammable and explosive gaseous acetylene, low-cost catalyst, wide substrate scope, satisfactory yield, and simple manipulation. This method can also be extended to gram scale.