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

Wang Gang | Zendy; Liu HaoBin | Zendy; He ZhaoLin | Zendy

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

Author(s) -

Wang Gang,

Liu HaoBin,

He ZhaoLin

Publication year - 2025

Publication title -

european journal of organic chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.825

H-Index - 155

eISSN - 1099-0690

pISSN - 1434-193X

DOI - 10.1002/ejoc.202500267

Subject(s) - chemistry , annulation , quinone , primary (astronomy) , organic chemistry , combinatorial chemistry , medicinal chemistry , catalysis , physics , astronomy

Abstract 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(1 H )‐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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