http://rdf.ncbi.nlm.nih.gov/pubchem/patent/IT-1107233-B
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_b287fc2ec423dbe49b66a4d8ad03cd1e |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K- |
| filingDate | 1978-09-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 1985-11-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1985-11-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | IT-1107233-B |
| titleOfInvention | DERIVATIVES OF 9-HYDROXYELLYPTYCIN SUITABLE FOR THERAPEUTIC USE AND RELATED PRODUCTION PROCESS |
| abstract | Prepn. of ellipticine derivs. of formula (I) and their quat. salts (R1 is H or alkyl; R2 is H, alkyl, aryl, benzyl or benzoyl) comprises (a) condensing 5-methoxyindole with 2,5-hexanedione; (b) demethylating the resulting 6-methoxy-1,4-dimethoxycarbazole to form 6-hydroxy-1,4-dimethylcarbazole; (c) protecting the OH gp. by benzylation or benzoylation; (d) opt. metallating the resulting 6-benz(o)yloxy-1,4-dimethylcarbazole (II) and reacting with alkyl iodide to form the corresp. 9-alkyl-6-benz(o)yloxy-1,4-dimethyl-carbazole (III); (e) formylating (II) or (III) to form the 3-formyl deriv.; (f) condensing with aminoacetaldehyde dimethyl acetal to form the corresp. 3-(2,2-dimethoxyethyliminomethyl) deriv.; (g) cyclising this to form (I) where R1 = H or alkyl and r2 = benzyl or benzoyl; (h) saponifying (I; R2 = benzoyl) or hydrogenolysing (I; R2 = benzyl) to form (I; R2 = H); (i) opt. reacting (I; R2 = H) with an alkyl halide to form the corresp. 2-alkyl quat. halide; and (j) opt. converting this into another quat. salt Cpds. (I) and their quat. salts are antitumour agents (see GB1436080 and 1508388). The process gives high yields of high-purity products. |
| priorityDate | 1978-09-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 28.