http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1141628-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J75-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J5-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J75-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J5-00 |
| filingDate | 1967-06-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1969-01-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1141628-A |
| titleOfInvention | Novel 6-halo-9-ß,10-‡-steroids and a process for the manufacture thereof |
| abstract | 1,141,628. 6-Halo-9#,10α-steroids. F. HOFFMANN-LA ROCHE & CO. A.G. 9 June, 1967 [10 June, 1966], No. 26765/67. Heading C2U. Novel compounds which comprise the 3- keto-4-dehydro, 3-keto-4,6-bisdehydro, 3-keto- 1,4 - bisdehydro, 3 - keto - 1,4,6 - trisdehydro, 3-acyloxy-3,5-bisdehydro, 3-(alkoxy, cycloalkyloxy, or aralkoxy) - 3,5 - bisdehydro and 3 - acyloxy - 2,4,6 - trisdehydro derivatives of a compound of formula (wherein R is C 1-6 alkyl and Hal is a F, Cl or Br atom which may be α- or #-orientated in the case of 3-keto-4-dehydro or 3-keto-1,4-bisdehydro derivatives) are prepared by halogenating at the 6-position a 3-keto-4-dehydro, 3-keto-4,6- bisdehydro or 3-(esterified or etherified hydroxy)-3,5-bisdehydro derivative of a compound of formula to yield a 3-keto-4-dehydro, 3-keto-4,6-bisdehydro, or 3-keto-4-dehydro derivative respectively of a compound of Formula I, and optionally subjecting this product to 1,2- and/or 6,7-dehydrogenation, or converting it into a 3- enol ether or 3-enol ester of the type formulated above in connection with Formula I. The 6-halogenation of a 3-keto-4,6-bisdehydro derivative of a compound of Formula II may be effected using chromyl chloride, with subsequent dehydration of the resulting 3-keto-4- dehydro-6-chloro-7-hydroxy compound, or using a peracid to obtain a 3-keto-4-dehydro- 6,7-epoxy compound which is treated with HF, HC1 or HI and dehydrated. When a mixture of 6α- and 6#-halo isomers is produced, these may be separated by chromatography and/or fractional crystallization, and the α-isomers may be isomerized to the # -isomers using an hydrohalic acid e.g. HC1 or HBr in acetic acid, ethanol, dioxan or chloroform. Pharmaceutical compositions comprise a compound of Formula I with a compatible carrier, and may be administered enterally, parenterally or rectally, as tablets, dragÚes, capsules, solutions, suspensions, emulsions and suppositories. The compounds of Formula I are stated to possess hormonal, specifically gestagenic or fertility-inhibiting, activity, and influence the gonadatrophin economy. |
| priorityDate | 1966-06-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 26.