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Optically active carbacyclin intermediates and processes for the preparation thereof

Assignee: Nisshin Seifun Group Inc
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Filing: 1988-12-19
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Granted: 1989-12-05
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Expires: 2008-12-19
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Abstract

Abstract New intermediate, an optically active (1S,5R)-7,7-alkylenedioxy-2-alkoxycarbonylbicyclo[3.3.0]octan-3-one which is useful for the synthesis of an optically active carbacyclin. This intermediate is prepared, as a non-reduced compound, from a racemic compound, (1SR,5RS)-7,7-alkylenedioxy-2-alkoxycarbonyl-cis-bicyclo[3.3.0]octan-3-one, by treatment of the racemic compound with a microorganism. The microorganism has an ability of specifically reducing the keto group of the (1R,5S) epimer of the racemic compound.

Inventors

  • 👤 Kenji Mori
  • 👤 Masahiro Tsuji

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-29 11:31
CPC Classifications
C; C07; C07D; C07D317/00; C07D317/08; C07D317/72; C12; C12N; C12N1/00; C12N1/14; C12N1/16; C12N1/165; C12N1/18; C12N1/185; C12P; C12P17/00; C12P17/02; C12P41/00; C12P41/002; C12R; C12R2001/00; C12R2001/645; C12R2001/84; C12R2001/85

Claims Analysis

Total Claims: 8
Claim 1
Independent Claim 124 words
A process for preparing a compound of formula (I) ##STR14## wherein R represents lower alkyl and B represents an alkylene group optionally substituted with alkyl, and a compound of formula (III) ##STR15## wherein R and B have the meanings given above, said process comprising treating a (1SR,5RS)-7,7-alkylenedioxy-2-alkoxycarbonyl-cis-bicyclo[3.3.0]octan-3-one, which is a racemic compound of formula (II) ##STR16## wherein R and B have the meanings given above, with a microorganism having an ability of specifically reducing the keto group of the (1R,5S) epimer of the racemic compound (II), thereby giving, as a nonreduced compound, an optically active (1S,5R)-7,7-alylenedioxy-2-alkoxy-carbonyl-bicyclo[3.3.0]octan-3-one of said formula (I) and, as a reduced compound, an optically active (1S,5R,6R,7S)-3,3-alkylenedioxy-7-hydroxy-6-alkoxycarbonylbicyclo [3.3.0] octane of said formula (III), wherein R ad B have the meanings given above.
Claim 2
Dependent Claim 124 words
A process for preparing a compound of formula (I) ##STR14## wherein R represents lower alkyl and B represents an alkylene group optionally substituted with alkyl, and a compound of formula (III) ##STR15## wherein R and B have the meanings given above, said process comprising treating a (1SR,5RS)-7,7-alkylenedioxy-2-alkoxycarbonyl-cis-bicyclo[3.3.0]octan-3-one, which is a racemic compound of formula (II) ##STR16## wherein R and B have the meanings given above, with a microorganism having an ability of specifically reducing the keto group of the (1R,5S) epimer of the racemic compound (II), thereby giving, as a nonreduced compound, an optically active (1S,5R)-7,7-alylenedioxy-2-alkoxy-carbonyl-bicyclo[3.3.0]octan-3-one of said formula (I) and, as a reduced compound, an optically active (1S,5R,6R,7S)-3,3-alkylenedioxy-7-hydroxy-6-alkoxycarbonylbicyclo [3.3.0] octane of said formula (III), wherein R ad B have the meanings given above.
Claim 3
Dependent Claim 26 words
The process of claim 1 which further comprises separating the compound of the formula (I) or the compound of the formula (III) by ordinary separation techniques.
Claim 4
Dependent Claim 17 words
The process of claim 1 wherein the microorganism for the treatment of the racemic compound is yeast.
Claim 5
Dependent Claim 13 words
The process of claim 3 wherein the yeast includes genera Pichia and Saccharomyces.
Claim 6
Dependent Claim 20 words
The process of claim 4 wherein the yeast includes Saccharomyces cerevisiae, Saccharomyces uvarum, Saccharomyces carlsbergensis, Saccharomyces bailii or Pichia terricola.
Claim 7
Dependent Claim 146 words
A process for converting a compound of formula III ##STR17## wherein R represents lower alkyl and B represents an alkylene group optionally substituted with alkyl, into a compound of formula II ##STR18## wherein R and B have the meanings given above, said process comprising subjecting to an oxidation reaction, an optically active (1S,5R,6R,7S)-3,3-alkylenedioxy-7-hydroxy-6-alkoxycarbonyl-bicyclo [3.3.0] octane of said formula III wherein R and B have the meanings given above, so as to convert the hydroxy group thereof into a keto group, subjecting the thus oxidized compound to saponification and decarboxylation so as to give a 7,7-alkylenedioxy-cis-bicyclo [3.3.0] octan-3-one of formula (IV) ##STR19## wherein B has the meaning given above, and introducing an alkoxycarbonyl group into the 2-position of the compound of formula (IV) to convert into the racemic compound, a (1SR,5RS)-7,7-alkylenedioxy-2-alkoxycarbonyl-cis-bicyclo [3.3.0] octan-3-one of said formula II wherein R and B have the meaning s given above.
Claim 8
Dependent Claim 146 words
A process for converting a compound of formula III ##STR17## wherein R represents lower alkyl and B represents an alkylene group optionally substituted with alkyl, into a compound of formula II ##STR18## wherein R and B have the meanings given above, said process comprising subjecting to an oxidation reaction, an optically active (1S,5R,6R,7S)-3,3-alkylenedioxy-7-hydroxy-6-alkoxycarbonyl-bicyclo [3.3.0] octane of said formula III wherein R and B have the meanings given above, so as to convert the hydroxy group thereof into a keto group, subjecting the thus oxidized compound to saponification and decarboxylation so as to give a 7,7-alkylenedioxy-cis-bicyclo [3.3.0] octan-3-one of formula (IV) ##STR19## wherein B has the meaning given above, and introducing an alkoxycarbonyl group into the 2-position of the compound of formula (IV) to convert into the racemic compound, a (1SR,5RS)-7,7-alkylenedioxy-2-alkoxycarbonyl-cis-bicyclo [3.3.0] octan-3-one of said formula II wherein R and B have the meaning s given above.

References Cited (Backward Citations)

EP0101076A2 Cited
US4659671A Cited
US4629701A Cited
US4668628A Cited
US4814468A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1992-12-04 1993-06-05 1993-12-05 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1996-12-04 1997-06-05 1997-12-05 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2000-12-04 2001-06-05 2001-12-05 $7700.00 Window Closed / Lapsed

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