[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.
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页数：6
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