A remarkable rate acceleration of the one-pot three-component cyclo-condensation reaction at room temperature: An expedient synthesis of mitotic Kinesin Eg5 inhibitor monastrol

被引：47
作者：
Bose, DS [1 ]
Kumar, RK [1 ]
Fatima, L [1 ]
机构：
[1] Indian Inst Chem Technol, Fine Chem Lab, Hyderabad 500007, Andhra Pradesh, India
来源：
SYNLETT | 2004年 / 02期
关键词：
mitotic; monastrol; 3,4-dihydropyrimidin-2(1H)-ones; biginelli reaction;
D O I：
10.1055/s-2004-815416
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A general and practical route for the synthesis of 3,4-dihydropyrimidin-2(1H)-ones by a one-pot condensation of aldehydes, beta-ketoesters, and urea is described using trimethylsilyl-triflate (I mol%)-mediated cyclocondensation reaction at room temperature within IS minutes. Yields are significantly higher than utilizing classical Biginelli reaction conditions. Synthesis of Mitotic Kinesin Eg5 inhibitor monastrol has been achieved in 95% isolated yield.
引用
收藏
页码：279 / 282
页数：4
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