http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1366028-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_4acae202b6a15394281949545e70d2f6 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J75-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C- http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-57 |
| filingDate | 1972-12-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1974-09-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1366028-A |
| titleOfInvention | 13-alkyl-18,19-dinor-pregnadiones processes for their preparation and compositions incorporating them |
| abstract | 1366028 7-Methylpregna-4,9,11-trienes and 13-homologues thereof ROUSSEL-UCLAF 8 Dec 1972 [8 Dec 1971] 56650/72 Heading C2U The invention comprises compounds of formula wherein R is alkyl and R<SP>1</SP> is H, alkyl, hydroxy or carboxylic acyloxy. They may be prepared from compounds of Formula II infra by hydrolysis to give the corresponding 3-oxo-5(10), 9(11)-diene followed by hydroperoxidation (e.g. with O 2 /tertiary amine) to give the corresponding 3 - oxo - 11# - hydroperoxy - 4,9 - diene followed by reduction to give the corresponding 3 - oxo - 11# - hydroxy - 4,9 - diene followed by dehydration to give I. Compounds of formula (wherein K is a ketal group and R and R<SP>1</SP> are as above) are prepared from compounds of Formula VII infra either (i) by hydration by the successive actions of B 2 H 6 and H 2 O 2 to give a corresponding 17#-(1-hydroxyethyl) compound, oxidation of which yields 2(R<SP>1</SP> = H); or (ii) by direct oxidation, e.g. with H 2 O 2 , to give 2(R<SP>1</SP> = OH). The latter may then be 17- acylated, or may be dehydrated to give the corresponding 16-ene, alkylation of which gives 2(R<SP>1</SP> = alkyl). Compounds of formula are prepared from the corresponding 17-ones by the Wittig reaction. Thereafter a dialkyl ketal group may be replaced by a cyclic ketal group by hydrolysis to the corresponding 3-one followed by reketalization with a diol. In Example 1 a by-product of the Wittig reaction is 3 - methoxy - 7α - methyl - 19 - norpregna - 3,- 5(10),9(11),17(20)-tetraene. Compounds I are said to possess exogenous antiandrogenic, antihypophysial and antiestrogenic properties, and may be made up with carriers into pharmaceutical compositions for oral, parenteral and rectal administration. |
| priorityDate | 1971-12-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
| Predicate | Subject |
|---|---|
| isDiscussedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID458397310 |
Total number of triples: 13.