Intramolecular Ring-Opening of Oxetanes: Access to Functionalised Hydroxymethyl 2,3-Dihydroimidazo[1,2-c ]quinazolines

被引:5
作者
Bagal, Sharan K. [1 ]
Bodnarchuk, Michael S. [1 ]
King, Thomas A. [1 ]
McKerrecher, Darren [1 ]
Luo, Xuehong [2 ]
Wang, Peng [2 ]
Steward, Oliver R. [1 ]
机构
[1] AstraZeneca, Oncol R&D, Chem, Cambridge, England
[2] Pharmaron Beijing Co Ltd, 6 Taihe Rd BDA, Beijing, Peoples R China
关键词
oxetane ring-opening; intramolecular cyclization; imidazoquinazolines; one-pot synthesis;
D O I
10.1055/s-0039-1691578
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
An intramolecular oxetane ring-opening was developed, affording novel 2-(hydroxymethyl)-2,3-dihydroimidazo[1,2- c ]quinazolines from N -(3-methyloxetan-3-yl)quinazolin-4-amines under mild conditions. The resulting medicinally relevant tricyclic scaffolds were synthesised in good yields with diverse substituents. Moreover, reaction optimisation led to the development of a one-pot procedure.
引用
收藏
页码:502 / 506
页数:5
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