[5+1] Annulation of aza-o-Quinone Methides with Primary Amines: Construction of 3,4-Dihydroquinazolin-2(1H)-One Derivatives

被引：0

作者：

Wang, Gang ^{[1
]}

Liu, Hao-Bin ^{[1
]}

He, Zhao-Lin ^{[1
]}

机构：

[1] Wuhan Inst Technol, Sch Chem & Environm Engn, Hubei Key Lab Novel Reactor & Green Chem Technol, Key Lab Green Chem Proc,Minist Educ, Wuhan 430205, Peoples R China

来源：

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY | 2025年

基金：

中国国家自然科学基金;

关键词：

aza-o-quinone methides; primary amines; 5+1] annulation reaction; 3,4-dihydroquinazolin-2(1H)-one derivatives; SELECTIVE PDE7 INHIBITORS; SULFUR YLIDES; POTENT; SPIROQUINAZOLINONES; REACTIVITY; DESIGN;

D O I：

10.1002/ejoc.202500267

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A [5+1] annulation between in situ generated aza-o-quinone methides and primary amines has been developed. This methodology offers efficient access to diverse 3,4-dihydroquinazolin-2(1H)-one derivatives with yields ranging from 45 % to 99 %. The significance of this methodology is highlighted by its application to the synthesis of a potential CDK5 inhibitor, a bioactive compound.

引用

页数：6