C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 319/20 (2006.01) C07C 205/26 (2006.01) C07C 205/37 (2006.01) C07C 205/43 (2006.01) C07D 265/36 (2006.01) C07D 303/26 (2006.01) C07D 317/22 (2006.01) C07D 317/62 (2006.01) C07D 327/06 (2006.01) C07F 7/10 (2006.01)
Patent
CA 2195724
The invention relates to a method for the stereoselective preparation of a hetero-bicyclic alcohol enantiomer, characterized in that a substantially pure enantiomer of the general formula (see formula I) wherein X is O, S, NH or N- (C1-C4) alkyl; Y1 and Y2 are each independently hydrogen or substituents selected from halogen, (C1-C4) alkyl, (C1-C4) alkoxy, (C1-C4)-haloalkyl, formyl, nitro and cyano; the C*-atom has either the R or the S configuration; is prepared from a compound of the general formula (see formula II) wherein R1 is hydrogen or a suitable protective group and R2 is hydrogen or wherein R1 and R2 together form an optionally mono- or di- (C1-C3)alkyl substituted methylene bridge; by the following successive reaction steps: (i) reaction with a compound of the general formula (see formula III) wherein Z is a hydroxy group or a suitable leaving group, R3 is a hydroxy-protective group and R4 is a halogen atom; or wherein R3 and R4 together constitute a valence bond or a biradical of the formula -C(R11)2-O-, wherein R11 is a straight or branched (C1-C4)alkyl group and wherein the C*-atom has either the R or the S configuration; (ii) subjection of the compound formed to a deprotection/ring- closure reaction; (iii) optionally deprotection of the hydroxy group of the ring-closed product. The invention further relates to enantiomerically pure intermediates, the preparation of these intermediates and the preparation of a starting compound.
Buizer Nicolaas
Kruse Chris G.
Schenk Klara M.
Shadid Belal
Duphar International Research B.v.
Fetherstonhaugh & Co.
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