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【结 构 式】 
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【药物名称】S-30972-1 【化学名称】9-(4-Carboxybutyryloxy)-N-[2-(dimethylamino)ethyl]-5,6-dimethyl-6H-pyrido[4,3-b]carbazole-1-carboxamide dihydrochloride 【CA登记号】209617-63-0, 209617-97-0 (free base) 【 分 子 式 】C27H32Cl2N4O5 【 分 子 量 】563.48589 |
【开发单位】Servier (Originator) 【药理作用】ONCOLYTIC DRUGS, Apoptosis Inducers, DNA Topoisomerase II Inhibitors, DNA-Intercalating Drugs, Ellipticines |
合成路线1
The title hemiglutarate ester was synthesized by acylation of the known olivacine derivative (I) with glutaric anhydride (II) in pyridine, followed by conversion to the corresponding dihydrochloride salt.
| 【1】 Charton, Y.; Guilbaud, N.; Léonce, S.; Pierré, A.; Guillonneau, C.; Michel, A.; Atassi, G.; Kraus-Berthier, L.; Bisagni, E.; Synthesis of 9-O-substituted derivatives of 9-hydroxy-5, 6-dimethyl-6H-pyrido[4,3-b]carbazole-1-carboxylic acid (2-(dimethylamino)ethyl)amide and their 10- and 11-methyl analogues with improved antitumor activity. J Med Chem 1999, 42, 12, 2191. |
| 【2】 Guilbaud, N.; Bisagni, E.; Guillonneau, C.; Charton, Y.; Atassi, G.; Pierre, A. (ADIR et Cie.); Ellipticine derivs., their preparation and pharmaceutical compsns. containing them. EP 0850940; US 6162811 . |
Extended Information