http://rdf.ncbi.nlm.nih.gov/pubchem/patent/TW-381120-B
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_6f5033fcf56d5a13743728cc85a8dc3f |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-582 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D265-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C12P41-004 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D319-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D327-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C12P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D311-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C12P17-14 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D311-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D265-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12N9-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D311-76 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D311-58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D327-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D319-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D411-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12P- http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D291-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D319-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D- http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12P17-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12P17-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12P17-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D407-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12P41-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D419-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F7-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-04 |
| filingDate | 1993-12-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2000-02-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f99c5bee0783f0ef289f03f66efd65ab http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_77ad333b567a3f266e82f5fd74606f17 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_682034b1f51afdae49b05b4aa06c2283 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_23e266f421fa1fc8e2b826594da5b52d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_12d8eb7dbdfbf0ba71ef098a73e9cc3e |
| publicationDate | 2000-02-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | TW-381120-B |
| titleOfInvention | Enzymatic process for the stereoselective preparation of a hetero-bicyclic alcohol enantiomer |
| 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 II (wherein Y' is hydrogen or a substituent selected from chloro, fluoro and methyl; 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:(I) acylation of said racemate with an acylating agent under the influence of an enzyme having a stereoselective esterification activity, in an organic solvent system containing up to 0.6% of water or aqueous buffer, at room temperature or a slightly elevated temperature up to approx. 40 degree C, said acylating agent being (a) a carboxylic anhydride, selected from acetic anhydride, propionic anhydride, butyric anhydride, isobutyric anhydride, hexanoic anhydride, succinic anhydride and glutaric anhydride, or (b) a vinyl ester selected from vinyl acetate, vinyl propionate, vinyl butyrate and vinyl isobutyrate; said enzyme being selected from the following lipases: Aspergillus niger, Candida cylindracea, Candida lipolytica, Chromobacterium viscosum, Geotrichum candidum, Humicola lanuginosa, Mucor miehei, Mucor javanicus, Pig pancreatic lipase, Penicillium cyclopium, Penicillium roqueforti, Pseudomonas cepacia, Pseudomonas fluorescence, Rhizopus niveus, Rhizopus javanicus, Rhizopus arrhizus and Rhizopus dalemar;(ii) separation of the unesterified compound from the ester produced and isolation of the desired substantially pure alcohol enantiomer of formula II or of its ester;(iii) subjection of the ester produced to a hydrolysis under acid or basic conditions, at room temperature or elevated temperature, thus converting said ester into the corresponding alcohol enantiomer; and (iv) conversion of the undesired alcohol enantiomer into the starting alcohol racemate under the influence of a base under aprotic or under protic conditions, at a temperature between (and including) room temperatre and reflux temperature of the solvent used; under protic conditions said base being selected from sodium hydroxide, potassium hydroxide, lithium hydroxide and ammonium hydroxide, dissolved in water or in an aqueous solvent mixture; under aprotic conditions said base being selected from sodium hydride, potassium alkoxides and alkyl lithium compounds, in an aprotic organic solvent.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 derivatives, and to substantially pure enantiomeric intermediates. |
| priorityDate | 1992-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 335.