Pd(II)-catalyzed cascade annulation of -substituted anilines with CO, NHOAc and aldehydes to 1-substituted 2,3-dihydroquinazolin-4(1)-ones.

Org Biomol Chem

NMPA Key Laboratory for Research and Evaluation of Innovative Drug, Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals, Key Laboratory of Green Chemical Media and Reactions, Ministry of Education, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang 453007, People's Republic of China.

Published: April 2024

A facile and direct approach to 1-substituted 2,3-dihydroquinazolin-4(1)-ones has been developed Pd(II)-catalyzed one-pot cascade annulation of -substituted anilines with CO, NHOAc and aldehydes, and it features an intrinsic directing strategy, cheap and easily obtainable raw materials, low cost, high step economy and efficiency, broad substrate scope and good product diversity. This protocol has been successfully applied to the synthesis of glycozolone A and gram-level experiments. Based on the control experiments and the literature, the reaction mechanism was proposed.

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http://dx.doi.org/10.1039/d4ob00055bDOI Listing

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