http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1368896-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_59e1d955a7b1560dc68cf7fd800e8fac |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D307-88 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D307-88 |
| filingDate | 1972-07-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1974-10-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1368896-A |
| titleOfInvention | Mycophenolic acid derivatives and process for production thereof |
| abstract | 1368896 Mycophenolic acid derivatives CHUGAI SEIYAKU KK 28 July 1972 [31 July 1971 (2) 24 Feb 1972] 35538/72 Heading C2A Novel mycophenolic acid derivatives having the Formula (I) wherein R is a C 1-6 alkyl group or a C 1-6 alkenyl group, and R<SP>1</SP> is (a) -NH 2 , in which X is hydrogen, halogen, hydroxy, carboxy, sulphamoyl, nitro, cyano, phenyl, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 2 -C 5 acyl, C 2 - C 5 alkoxycarbonyl, C 2 -C 5 acylamino, C 5 -C 7 dialkylaminoethoxycarbonyl, or C 2 -C 8 dialkylamino; X<SP>1</SP> and Y<SP>1</SP> are the same or different and each is hydroxy, nitro, carboxy or C 1 -C 4 alkyl; and X<SP>2</SP> is hydrogen, halogen or C 2 -C 8 dialkylamino, are prepared by either (i) reacting an R- esterified mycophenolic acid haloformate of Formula (II) in which R is as defined above and X<SP>3</SP> is halogen, with an amine of formula HR<SP>1</SP>; or (ii) when R<SP>1</SP> is -NH 2 , by reacting a mycophenolic acid ester of Formula (IV) in which R is as defined above, with a metal salt of cyanic acid. The reactions may be carried out in an inert solvent or in an excess of one of the reactants. Reaction (i) is preferably conducted in the presence of an acid binding agent, e.g. a tertiary organic amine which may be an excess of the amine of formula HR<SP>1</SP> or sodium or potassium bicarbonate. Reaction (ii) is preferably carried out in the presence of a strong acid (e.g. HCl, H 2 SO 4 or a trihalogenoacetic acid) using sodium or potassium cyanate. Any reactive or labile substituents in the amine HR<SP>1</SP> may be suitably protected before the preparative reaction. Compounds of Formula (II) above are prepared by subjecting mycophenolic acid to a conventional esterification procedure and then reacting the ester with phosgene. Pharmaceutical compositions having anticancer and anti-tumour activity comprise a mycophenolic acid derivative of Formula (I) hereinbefore, together with a pharmaceutically acceptable carrier or diluent. |
| priorityDate | 1971-07-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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