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Updated: Jun 4, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
One-Step Construction of 2-Methylquinazolin-4(3H)-ones Using Solid Calcium Carbide as an Alternative to Gaseous
Botao Wang1, Zhiqiang Wang1, Xinjie You1
1College of Chemistry and Chemical Engineering, Northwest Normal University, Lanzhou, Gansu 730070, P. R. China.
Abstract:
2-Methylquinazolin-4(3H)-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.
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