http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-406543-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_4acae202b6a15394281949545e70d2f6 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J63-008 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-568 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-565 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J1-0096 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J1-0092 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-57 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C- http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J13-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-565 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J51-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K- http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J71-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-575 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J9-00 |
| filingDate | 1972-09-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1975-09-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-406543-A1 |
| titleOfInvention | A PROCEDURE FOR THE PREPARATION OF 3,16 ALPHA, 17 XI-TRIHI- DROXI-11 BETA -ALCOXI-ESTRA-1,3,5 (10) -TRIENS. |
| abstract | A method of preparing the 3,16α, 17 ξ -trihydroxy-11β-alkoxy-estra-1,3,5 (10) -triene of general formula I: **(See formula)** in which X represents a methyl or ethyl radical; R represents hydrogen or an unsaturated hydrocarbon radical having 2 to 4 carbon atoms; R1 represents hydrogen or the acyl moiety of an organic carboxylic acid having 1 to 18 carbon atoms; R2 represents hydrogen, the acyl residue of an organic carboxylic acid having 1 to 18 carbon atoms, when R is hydrogen, or R2 represents with R3, when the OR2 and OR3 groups have the same spatial orientation, the rest of a alcoholicidene or aralkohilidene group of the form (see formula) in which A is hydrogen or a hydrocarbon radical and B is a hydrocarbon radical; R3 represents hydrogen, the acyl moiety of an organic carboxylic acid having 1 to 13 carbon atoms, or R3 represents with R2, when the OR2 and OR3 groups have the same spatial orientation, the rest of an alcoholidene or aralkohylidene group, the wavy line indicating that the orientation of the α or β substituents characterized in that an 11β-alkoxystrone, in which the alkoxy radical has 1 or 2 carbon atoms, is subjected to the action of an acylating agent in an acid medium to obtain a 3,17-diacyloxy-11β-alkoxy-estra 1,3,5 (10) 16-tetraene of general formula **(See formula)** in which Ac represents the acyl residue of an organic carboxylic acid having one to eighteen carbon atoms and X maintains the same meaning as above, it is treated with an organic peracid to obtain a 3,17β-diacyloxy-11β-alkoxy-16α, 17α-epoxy-estra-1,3,5 (10) -triene of general formula III: **(See formula)** in which Ac and X are defined as above, the epoxide is hydrolyzed in an acidic medium to obtain the 3,16α-dihydroxy-11β-alkoxy-17-oxo-estra-1,3,5 (10) -triene of general formula IV: **(See formula)** in which X is defined as above, the compound of formula IV is subjected either to the action of an alkaline reducing agent, obtaining 3.16α 17β-trihydroxy-11β-alkoxy-estra-1,3,5 (10) -triene sought and, if appropriate, said product is esterified in position 3 or in positions 3, 16 and 17 by the action of an organic carboxylic acid having 1 to 18 carbon atoms, or one of its functional derivatives ; or, after possible esterification with an organic carboxylic acid having from 1 to 18 carbon atoms or one of its functional derivatives, to the action of a hydrocarbonylation reagent whose hydrocarbonyl radical R is defined as above, is carried out in the case from a diacylated derivative at positions 3 and 16α the saponification of the hydrocarbonyl derivatives at position 17 thus obtained, in alkaline medium, 3.16α, 17α-trihydroxy-11β-alkoxy-17α-R-estra-1 are obtained, 3,5 (10) -triene and the 3,16α, 17β-trihydroxy-11β-alkoxy-17α-R-estra-1,3,5 (10) -triene sought, and, if applicable, these are esterified products in position 3 or in positions 3 and 16 by the action of an organic carboxylic acid having 1 to 18 carbon atoms or one of its functional derivatives, or, where appropriate, when the hydroxyls in positions 16 and 17 have the same spatial orientation, a ketone is formed by condensation with a ketone or an aliphatic or arylaliphatic aldehyde co in the presence of a mineral or organic acid. (Machine-translation by Google Translate, not legally binding) |
| priorityDate | 1971-09-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 37.