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.
|Number of pages||4|
|Publication status||Published - 13 Nov 2001|