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1. 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.

2. 发明专利

DE69714875D1 未知
公开(公告)号：DE69714875D1
公开(公告)日：2002-10-02
申请号：DE69714875
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.

3. 发明专利

AT222902T 未知
公开(公告)号：AT222902T
公开(公告)日：2002-09-15
申请号：AT97200185
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.

4. 发明专利

AU701883B2 Process for the stereoselective preparation of a hetero-bicyclic alcohol enantiomer 未知
公开(公告)号：AU701883B2
公开(公告)日：1999-02-11
申请号：AU1001897
申请日：1997-01-02
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 , C07D303/23 , C07D317/22
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.

5. 发明专利

AU1001897A Process for the stereoselective preparation of a hetero-bicyclic alcohol enantiomer 未知
公开(公告)号：AU1001897A
公开(公告)日：1997-07-31
申请号：AU1001897
申请日：1997-01-02
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 , C07D303/23 , C07D317/22
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

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.

7. 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.

8. 发明专利

HK1000698A1 PROCESS FOR THE PREPARATION OF A HETERO-BICYCLIC ALCOHOL ENANTIOMER 未知
公开(公告)号：HK1000698A1
公开(公告)日：2002-12-13
申请号：HK97102232
申请日：1997-11-22
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 , C07D , C07C
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.

9. 发明专利

CZ20697A3 PROCESS OF STEREOSELECTIVE PREPARATION OF HETEROBICYCLIC ALCOHOL ENANTIOMER 未知
公开(公告)号：CZ20697A3
公开(公告)日：1997-08-13
申请号：CZ20697
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

NO970281A 未知
公开(公告)号：NO970281A
公开(公告)日：1997-07-28
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
CPC分类号： C07D317/62 , C07C41/16 , C07C67/08 , C07C67/287 , C07C201/08 , C07C201/12 , C07D265/36 , C07D319/20 , C07D327/06 , C07F7/1852 , Y02P20/55 , C07C205/43 , C07C205/37 , C07C205/35 , C07C205/26 , C07C69/16 , C07C69/28 , C07C69/78 , C07C69/017 , C07C43/23 , C07C69/63

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