http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1022209-A
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_dc2f7134efa50484bb359fda73782848 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J53-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J75-00 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J53-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J75-00 |
filingDate | 1962-10-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 1966-03-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | GB-1022209-A |
titleOfInvention | Cyclosteriods and process for their manufacture |
abstract | The invention comprises (1) a process for the preparation of 9b ,19-cyclosteroids which comprises esterifying a 19-hydroxy-steroid having an 11-oxo group or a 9(11)-double bond with a sulphonic acid, treating the ester so obtained with a basic agent to give an 11-oxo- or D 11(12)-9b ,19-cyclosteroid and, if desired, splitting off the 11-oxo group with hydrazine in a known manner or hydrogenating the 11,12-double bond; and (2) 9b ,19-cyclosteroids of the partial formulae <FORM:1022209/C2/1> wherein R is two hydrogen atoms or an oxo group and X is hydrogen, methyl, fluorine or chlorine, and belonging to the androstane, pregnane, cholane, spirostane, cholestane or cardanolide series. If the product of (1) contains a free or protected 3-hydroxyl group or a protected 3-oxo group, this group may be converted into a 3-oxo group, and if the compound so obtained is ring A saturated, a D 4-double bond may be introduced by bromination and dehydrobromination. 20-keto groups may also be released from 20-ketals. Suitable starting materials for process (1) are of the above-mentioned series, as well as triterpenenes, e.g. of the lanostane type. They may have alkyl, alkenyl, alkyryl, free, esterified or etherified hydroxyl or free or functionally modified keto (e.g. ketals, enamines or enol ethers) groups or halogen atoms as substituents in the nucleus or side chains, and may also have one or more double bonds, e.g. in ring D or the 17-side chain. Examples are given. D 9(11) - 3,20 - ethylenedioxy - 19 - hydroxy-5a - pregnane is prepared by reducing 3,20-ethylenedioxy - 11 - oxo - 19 - hydroxy - 5a -pregnane to 3,20-ethylenedioxy-11b ,19-dihydroxy-5a -pregnane, converting this to the 19-acetate, dehydrating this to D 9'11'-3,20-ethylenedioxy-19-acetoxy-5a -pregnane, and hydrolysing this. These processes are also referred to in more general terms. The 9b ,19-cyclosteroids of the invention, which variously have sodium-eliminating, progestational, anabolic, anti-inflammatory and anti-shock properties, may be made up into pharmaceutical compositions with suitable carriers. These may take the form of solutions, suspensions, emulsions, implants, tablets, dragees, ointments or creams, and may contain preserving, stabilizing, wetting or emulsifying agents, salts for varying the osmotic pressure, or buffers. |
priorityDate | 1961-10-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 42.