http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1534733-A2
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_49cd70b288ee3892f04f8e1b9f4f33d3 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J3-005 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J31-006 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J41-0038 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J41-00 |
filingDate | 2003-06-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_36033b54716a6783813bb3da9088f7de http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_32f86c5c174b530f75d5749f5f7a741b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0ccb2707b3d66ac6a635ce4f92fb93aa http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fcd80727a38334ea5ed1bf9ec9bae6af |
publicationDate | 2005-06-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | EP-1534733-A2 |
titleOfInvention | Convenient synthesis of s-fluoromethyl 6alpha, 9alpha-difluoro-11beta-hydroxy-16alpha- methyl-17alpha-propionyloxy-3-oxoandrosta-1, 4-diene-17beta-carbothioate |
abstract | The present invention provides a convenient process for the preparation of S-fluoromethyl 6a, 9a-difluoro-11b-hydroxy-16a-methyl-17a-propionyloxy-3-oxoandrosta-1, 4-diene-17b-carbothioate, a compound of formula (1), comprising(a) treating 17b-[(N, N-dimethylcarbamoyl)thio]carbonyl-6a,9a-difluoro-11b-hydroxy-16a-methyl-17a-propionyloxy-3-oxoandrosta-1, 4-diene, a compound of formula (3) with alkali metal carbonate-alcohol system to obtain 6a, 9a-difluoro-11b-hydroxy-16a-methyl-17a-propionyloxy-3-oxoandrosta-1, 4-diene-17b-carbothioic acid, a compound of formula (4); (b) reacting the compound of formula (4) with bromofluoromethane to yield the compound of formula (1).The present invention also provides an improved process for preparation of compound of formula (1) comprising (a) reacting 6a, 9a-difluoro-11b-hydroxy-16a-methyl-3-oxo-17a-(propionyloxy) androsta-1, 4-dien-17b-carboxylic acid, a compound of formula (2), with N,N-dimethylthiocarbamoyl chloride in an inert aprotic solvent in the presence of an iodide catalyst and a base to give a compound of formula (3), (b) reacting the compound of formula (3) with a hydrosulfide reagent and bromofluromethane to obtain a compound of formula (1). |
priorityDate | 2002-06-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 125.