http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2663484-C1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_99cd2888b2026702c522c60b1544ff90 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J5-0053 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J75-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J75-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J5-00 |
| filingDate | 2017-05-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2018-08-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3f1eb5af7276136b8bd895dd3419aa04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b2c036cbd8d1769925c96895acd1ff6f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_83fb4394d6e47bd51c3d7b48cf3c7ec6 |
| publicationDate | 2018-08-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | RU-2663484-C1 |
| titleOfInvention | METHOD OF PREPARATION 6α-METHYLHYDROCORTISONE OR ESTERS THEREOF FROM HYDROCORTISONE 21-ACETATE |
| abstract | FIELD: chemistry. n SUBSTANCE: invention relates to a process for the preparation of 6α-methylhydrocortisone (11β, 17α, 21-trihydroxy-6α-methylpregn-4-ene-3,20-dione) or esters thereof of general formula I I, in which R=COCF 3 or H; R 1 =COCH 3 or H, from hydrocortisone 21-acetate of formula II, through a series of conversions, comprising protection of the 11β-hydroxyl group by esterification with a trifluoroacetic acid derivative in an aprotic solvent under basic catalysis conditions to form 21-acetoxy-17α-hydroxy-11β-trifluoroacetyloxypregn-4-ene-3,20-dione of formula III, enol-esterification of a Δ 4 -3-keto system of the resulting compound by the action of a trialkyl orthoformate in the presence of an acidic catalyst to form a 3-alkoxyester of a Δ 3,5 -3-hydroxy derivative of general formula IV, condensing it with a Mannich reagent in the presence of an acid catalyst to form a mixture of 6α- and 6β-isomers of 6-(N-methyl-N-phenyl)-aminomethyl derivative of general formula V, cleavage of the resulting mixture of steroid Mannich bases on the C-N bond with the action of a mineral acid in the presence of hydrohalic acid salts to form a 6-methylene derivative of formula VI, isomerisation of the 6-exomethylene bond to the 6,7-endomethylene bond to form compound VII; catalytic hydrogenation of the 6,7-endomethylene bond to form a mixture of 6α-methyl- and 6β-methyl isomers and subsequent isomerisation of 6β-methyl isomer to a 6α-methyl derivative of formula VIII, removal of protective groups 11β- and 21-hydroxyl groups entirely or in part. II, III, IV, V, VI, VII, VIII. n EFFECT: simple method for preparing a compound of formula I from hydrocortisone 21-acetate with output of desired products not less than 80 %. n 23 cl, 12 ex |
| priorityDate | 2017-05-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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