http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1477997-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_eccd894c99fea2d1c0c8735872bb2309 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C43-295 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C67-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C255-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-085 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C255-37 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C41-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C43-295 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C27-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C253-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C33-46 |
| filingDate | 1976-04-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1977-06-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1477997-A |
| titleOfInvention | Phenylalkanols and their preparation |
| abstract | 1477997 Phenylalkanols MERCK PATENT GmbH 30 April 1976 [2 May 1975] 17805/76 Heading C2C Novel compounds of the Formula I wherein Ar is unsubstituted phenyl or a phenyl mono- or di-substituted by F, Cl, Br and/or methyl, X is F, Cl, Br or cyano, m is 0 or 1 and n is 2 or 3, may be prepared by (1) hydrolysis of a compound II wherein Q is metal alcoholate, ester, ether, Cl, Br or I; (b) converting the amino group in the compound III into F, Cl or Br via a diazonium salt, (c) reacting a compound IV wherein E is a free or esterified hydroxyl, with an inorganic halide or cyanide, (d) reacting an appropriate 2 - X - propionyl- or a 3 - X- butyryl benzene with methyl magnesium halide, (e) reacting an Ar(O) m substituted acetophenone with an X substituted ethyl or propyl lithium compound, (f) reacting an Ar(O) m substituted phenyl magnesium halide with a 1 - X - substituted - butan - 3 - one or pentan- 4 - one, (g) converting chloro or bromo at X to F or CN using an inorganic fluoride or cyanide or (h) chlorinating or brominating a compound I in which Ar is unsubstituted or monosubstituted with Cl or Br. 4 - (2 - Chloropropionyl) - 4<SP>1</SP>- fluorobiphenyl is prepared by reacting 4-fluorobiphenyl with 2- chloropropionyl chloride under Friedel Craft conditions. The 1 - X - substituted - 3 - (4<SP>1</SP>- amino - 4- biphenylyl) - butan - 3 - ols are prepared by nitration followed by reduction or the corresponding 1 -X-3-(4-biphenylyl)-butan-3-ol. 3 - (41 - Fluoro - 4 - biphenyl) - butane - 1,3- diol is prepared by reacting 4-fluorophenylacetophenone with ethyl bromoacetate/zinc (Reformatsky) and reducing the 3-(4<SP>1</SP> fluoro-4- biphenylyl) - 3 - hydroxybutyric acid ethyl ester formed. The diol was converted to its 1-ptoluene sulphonate, 1-methane sulphonate and 1-benzene sulphonate. Pharmaceutical compositions of the compounds I with the usual excipients show anti-inflammatory and liver enzyme inducing activity, reduce the cholesterol, triglyceride and uric acid levels and inhibit thrombocyte aggregation when administered enterally, parenterally or topically. |
| priorityDate | 1975-05-02-04:00^^<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: 57.