期刊
TETRAHEDRON LETTERS
卷 43, 期 34, 页码 5913-5916出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0040-4039(02)01269-8
关键词
multicomponent reaction; Biginelli reaction; 3,4-dihydropyrimidine-2-thione; monastrol
The Yb(OTf)(3) catalyzed Biginelli cyclocondensation reaction of 3-hydroxybenzaldehyde, ethyl acetoacetate and thiourea afforded the corresponding dihydropyrimidine-2-thione, called monastrol, in 95% isolated yield. The chiral resolution of racemic monastrol, a mitosis blocker by kinesin Eg5 inhibition, was carried out on a preparative scale (ca. 100 mg) through diastereomeric N-3 ribofuranosyl amides. (C) 2002 Elsevier Science Ltd. All rights reserved.
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