http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2663483-C1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_99cd2888b2026702c522c60b1544ff90 |
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/C07J5-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J75-00 |
filingDate | 2017-12-29-04:00^^<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_83fb4394d6e47bd51c3d7b48cf3c7ec6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b2c036cbd8d1769925c96895acd1ff6f |
publicationDate | 2018-08-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | RU-2663483-C1 |
titleOfInvention | Method of preparing 6-(n-methyl-n-phenyl)aminomethyl-hydrocortisone esters thereof from hydrocortisone 21-acetate |
abstract | FIELD: chemistry.SUBSTANCE: invention relates to a method of producing 6-(N-methyl-N-phenyl)aminomethyl-hydrocortisone (11β,17α,21-trihydroxy-6-(N-methyl-N-phenyl)aminomethylpregn-4-ene-3,20-dione) or esters thereof of general formula I,in which R=COCFor H; R=COCHor H, from hydrocortisone 21-acetate of formula II, a sequence of transformations, including protection 11β-hydroxyl group by esterification with a trifluoroacetic acid derivative in an aprotic solvent medium under conditions of basic catalysis using an effective amount of a catalyst to form 21-acetoxy-17α-hydroxy-11β-trifluoroacetoxypregn-4-ene-3,20-dione of formula III, enol-esterification Δ-3-keto system of the obtained compound by the action of a trialkyl orthoformate in the presence of an acid catalyst to form a 3-alkoxyester Δ-3-hydroxy derivative of general formula IV, condensing it with Mannich reagent, formed in situ from formaldehyde and N-methylaniline, in the presence of an acid catalyst and deprotection of 11β- and 21-hydroxyl groups by methods of chemical solvolysis completely (R=R=H) or partially (R=H; R=COCH).,,.EFFECT: method has been developed for the preparation of compounds of formula I from hydrocortisone 21-acetate with the yield of the desired products of at least 85 %.34 cl, 7 ex |
priorityDate | 2017-12-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 116.