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2. 发明专利

JPH09216878A STEREOSELECTIVE PRODUCTION OF MIRROR IMAGE ISOMER OF HETEROCYCLIC BICYCLIC ALCOHOL 失效
公开(公告)号：JPH09216878A
公开(公告)日：1997-08-19
申请号：JP2190397
申请日：1997-01-22
申请人： DUPHAR INT RES
发明人： BUIZER NICOLAAS , KRUSE CHRIS G , SCHENK KLARA M , SHADID BELAL
IPC分类号： C07D317/48 , C07C205/22 , C07C205/26 , C07C205/37 , C07C205/43 , C07C217/84 , C07D265/00 , C07D265/36 , C07D279/16 , C07D303/20 , C07D317/62 , C07D319/20 , C07D327/06
摘要： 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 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 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 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.

3. 发明专利

CA2195724C PROCESS FOR THE STEREOSELECTIVE PREPARATION OF A HETERO-BICYCLIC ALCOHOL ENANTIOMER 未知
公开(公告)号：CA2195724C
公开(公告)日：2006-05-16
申请号：CA2195724
申请日：1997-01-22
申请人： DUPHAR INT RES
发明人： BUIZER NICOLAAS , KRUSE CHRIS G , SCHENK KLARA M , SHADID BELAL
IPC分类号： C07D317/48 , C07D319/20 , C07C205/22 , C07C205/26 , C07C205/37 , C07C205/43 , C07C217/84 , C07D265/00 , C07D265/36 , C07D279/16 , C07D303/20 , C07D303/26 , C07D317/22 , C07D317/62 , C07D327/06 , C07F7/10
摘要： The invention relates to a method for the stereoselective preparation o f 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.

4. 发明专利

CZ286162B6 Process for preparing enantiomer piperazine derivative 未知
公开(公告)号：CZ286162B6
公开(公告)日：2000-01-12
申请号：CZ290597
申请日：1997-09-15
申请人： DUPHAR INT RES
发明人： BUIZER NICOLAAS , KRUSE CHRIS G , VAN DER LAAN MELLE , LANGRAND GEORGES , VAN SCHARRENBURG GUSTAAF J M , SNOEK MARIA C
IPC分类号： C12P41/00 , C07D20060101 , C07D265/36 , C07D291/08 , C07D311/04 , C07D311/58 , C07D311/76 , C07D319/16 , C07D319/20 , C07D327/06 , C07D405/04 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/12 , C07D411/10 , C07D413/04 , C07D413/10 , C07D413/14 , C07D419/10 , C07F7/10 , C12N9/14 , C12P20060101 , C12P17/00 , C12P17/06 , C12P17/14 , C12P17/16 , C12P17/18
摘要： In the present invention there is disclosed a process for preparing a substantially pure enantiomer piperazine derivative of the general formula IX, in which X represents oxygen, sulfur, the group NH, N-alkyl containing 1 to 4 carbon atoms or CHi2, Yi1, Yi2 and Yi3 each represents hydrogen, a halogen alkyl containing 1 to 4 carbon atoms , alkoxyl containing 1 to 4 carbon atoms, haloalkyl containing 1 to 4 carbon atoms a nitro group or a cyano group, A represents alkylene containing 2 to 4 carbon atoms, B represents an optionally substituted phenyl or heterocyclic group and C*-atom is in R-configuration. The invented process is characterized in that (a) a racemic alcohol of the general formula I is acylated with an acylating agent in the presence of an enzyme exhibiting stereoselective esterification activity, the non-esterified compound is separated from the formed ester that is subsequently subjected to hydrolysis and a waste undesired alcohol enantiomer is then converted under basic conditions to the starting racemic alcohol that is brought again back into reaction, (b) a free hydroxy group of so obtained alcohol enantiomer is protected, (c) a nitro group of the product is reduced to an amino group, (d) the amino compound is then converted to a piperazine compound, (e) said piperazine compound is subsequently subjected to derivatization and (f) from the obtained compound the protecting group is cleaved.

5. 发明专利

NZ314103A STEREOSELECTIVE PREPARATION OF HETEROBICYCLIC ALCOHOL ENANTIOMER; INTERMEDIATES 未知
公开(公告)号：NZ314103A
公开(公告)日：1997-12-19
申请号：NZ31410397
申请日：1997-01-22
申请人： DUPHAR INT RES
发明人： BUIZER NICOLAAS , KRUSE CHRIS G , SCHENK KLARA M , SHADID BELAL
IPC分类号： C07D317/48 , C07C205/22 , C07C205/26 , C07C205/37 , C07C205/43 , C07C217/84 , C07D265/00 , C07D265/36 , C07D279/16 , C07D303/20 , C07D317/62 , C07D319/20 , C07D327/06 , C07D319/00
摘要： 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 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 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 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.

6. 发明专利

CA2195724A1 PROCESS FOR THE STEREOSELECTIVE PREPARATION OF A HETERO-BICYCLIC ALCOHOL ENANTIOMER 未知
公开(公告)号：CA2195724A1
公开(公告)日：1997-07-26
申请号：CA2195724
申请日：1997-01-22
申请人： DUPHAR INT RES
发明人： BUIZER NICOLAAS , KRUSE CHRIS G , SCHENK KLARA M , SHADID BELAL
IPC分类号： C07D317/48 , C07C205/22 , C07C205/26 , C07C205/37 , C07C205/43 , C07C217/84 , C07D265/00 , C07D265/36 , C07D279/16 , C07D303/20 , C07D317/62 , C07D319/20 , C07D327/06 , C07F7/10 , C07D317/22 , C07D303/26
摘要： 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 fig I) (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 fig. II) (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 fig. III) (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/ringclosure 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 intenmediates and the preparation of a starting compound.

7. 发明专利

HU9700200D0 PROCESS FOR THE STEREOSELECTIVE PREPARATION OF A HETERO-BICYCLIC ALCOHOL ENANTIOMER 未知
公开(公告)号：HU9700200D0
公开(公告)日：1997-03-28
申请号：HU9700200
申请日：1997-01-22
申请人： DUPHAR INT RES
发明人： BUIZER NICOLAAS , KRUSE CHRIS G , SCHENK KLARA M , SHADID BELAL
IPC分类号： C07D317/48 , C07C205/22 , C07C205/26 , C07C205/37 , C07C205/43 , C07C217/84 , C07D265/00 , C07D265/36 , C07D279/16 , C07D303/20 , C07D317/62 , C07D319/20 , C07D327/06
摘要： 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 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 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 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.

8. 发明专利

NO934652L 未知
公开(公告)号：NO934652L
公开(公告)日：1994-06-22
申请号：NO934652
申请日：1993-12-16
申请人： DUPHAR INT RES
发明人： BUIZER NICOLAAS , KRUSE CHRIS G , VAN DER LAAN MELLE , LANGRAND GEORGES , VAN SCHARRENBURG GUSTAAF J M , SNOEK MARIA C
IPC分类号： C12P41/00 , C07D20060101 , C07D265/36 , C07D291/08 , C07D311/04 , C07D311/58 , C07D311/76 , C07D319/16 , C07D319/20 , C07D327/06 , C07D405/04 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/12 , C07D411/10 , C07D413/04 , C07D413/10 , C07D413/14 , C07D419/10 , C07F7/10 , C12N9/14 , C12P20060101 , C12P17/00 , C12P17/06 , C12P17/14 , C12P17/16 , C12P17/18
摘要： The invention relates to substantially pure hetero-bicyclic alcohol enantiomers of the formula I, III, and IV 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 configuration. The invention also relates to the use of said enantiomers for the preparation of a pharmacologically active piperazine derivative.

9. 发明专利

NO315515B1 未知
公开(公告)号：NO315515B1
公开(公告)日：2003-09-15
申请号：NO970281
申请日：1997-01-22
申请人： DUPHAR INT RES
发明人： BUIZER NICOLAAS , KRUSE CHRIS G , SCHENK KLARA M , SHADID BELAL
IPC分类号： C07D317/48 , C07C205/22 , C07C205/26 , C07C205/37 , C07C205/43 , C07C217/84 , C07D265/00 , C07D265/36 , C07D279/16 , C07D303/20 , C07D317/62 , C07D319/20 , C07D327/06
摘要： 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 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 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 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.

10. 发明专利

DK0786459T3 未知
公开(公告)号：DK0786459T3
公开(公告)日：2003-01-06
申请号：DK97200185
申请日：1997-01-23
申请人： DUPHAR INT RES
发明人： BUIZER NICOLAAS , KRUSE CHRIS G , SCHENK KLARA M , SHADID BELAL
IPC分类号： C07D317/48 , C07C205/22 , C07C205/26 , C07C205/37 , C07C205/43 , C07C217/84 , C07D265/00 , C07D265/36 , C07D279/16 , C07D303/20 , C07D317/62 , C07D319/20 , C07D327/06
摘要： 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 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 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 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.

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