Synthesis and configuration of the cyclin-dependent kinase inhibitor roscovitine and its enantiomer

被引：37
作者：
Wang, SD
McClue, SJ
Ferguson, JR
Hull, JD
Stokes, S
Parsons, S
Westwood, R
Fischer, PM
机构：
[1] Cyclacel Ltd, Dundee DD1 5JJ, Scotland
[2] UFC Ltd, Manchester M15 6SY, Lancs, England
[3] Univ Edinburgh, Dept Chem, Edinburgh EH9 3JJ, Midlothian, Scotland
来源：
TETRAHEDRON-ASYMMETRY | 2001年 / 12卷 / 20期
关键词：
D O I：
10.1016/S0957-4166(01)00471-2
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
The cyclin-dependent kinase inhibitor (R)-2-(6-benzylamino-9-isopropyl-9H-purin-2-ylamino)butan-1-ol (roscovitine, 1a), as well as its (S)-enantiomer 1b, were synthesised. The chemical structure and absolute configuration of both enantiomers was confirmed by X-ray crystallography. Furthermore, high enantiomeric excess (>98%) was demonstrated by chiral chromatography of la and 1b, as well as NMR analysis of the diastereomeric Mosher's ester derivatives 2a and 2b. (C) 2001 Elsevier Science Ltd. All rights reserved.
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页码：2891 / 2894
页数：4
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