C - Chemistry – Metallurgy – 12 – P
Patent
C - Chemistry, Metallurgy
12
P
C12P 17/14 (2006.01) C07D 265/36 (2006.01) C07D 291/08 (2006.01) C07D 311/04 (2006.01) C07D 311/58 (2006.01) C07D 311/76 (2006.01) C07D 319/16 (2006.01) C07D 319/20 (2006.01) C07D 327/06 (2006.01) C07D 405/04 (2006.01) C07D 405/10 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01) C07D 407/12 (2006.01) C07D 411/10 (2006.01) C07D 413/04 (2006.01) C07D 413/10 (2006.01) C07D 413/14 (2006.01) C07D 419/10 (2006.01) C07F 7/10 (2006.01) C12N 9/14 (2006.01) C12P 17/00 (2006.01) C12P 17/06 (2006.01) C12P 17/16 (2
Patent
CA 2111607
Abstract The invention relates to an enzymatic process for the stereoselective preparation of a hetero-bicyclic alcohol enantiomer, characterized in that a substantially pure enantiomer of the general formula Image (I) wherein X is O, S, NH, N-(C1-C4)alkyl or CH2; Y1, Y2 and Y3 are each independently hydrogen or substituents selected from halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, nitro and cyano; the NO2 substituent is attached to the bicyclic ring system in the 5- or 7-position; and the C*-atom has either the R or the S configuration; is prepared from its corresponding alcohol racemate by the following successive reaction steps: (1) stereoselective esterification, (2) separation of the alcohol from the ester produced, (3) hydrolysis of said ester to produce the corresponding alcohol enantiomer, and (4) conversion of said alcohol enantiomer into the starting racemate under basic conditions in order to allow its reuse. The invention also relates to a substantially pure alcohol enantiomer of formula I, to the use of said enantiomer for the preparation of a pharmacologically active piperazine derivative, and to substantially pure enantiomeric intermediates.
Buizer Nicolaas
Kruse Chris G.
Langrand Georges
Van Der Laan Melle
Van Scharrenburg Gustaaf J.m.
Duphar International Research B.v.
Fetherstonhaugh & Co.
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