Process for preparing Topotecan from 10-hydroxy-4-(S) camptothecin
AssigneeCouncil of Scientific and Industrial Research
InventorsSatish Chander Puri, Geeta Handa, Kanaya Lal Dhar, Om Parkash Suri, Ghulam Nabi Qazi
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Abstract
The present invention relates to the use of dihalomethanes as reagents for the preparation of Topotecan{4-(S)-10(dimethylamino)-methyl-4-ethyl 4,9 dihydroxyl-H-pyrano[3′4′:6,7]indolizino-[1,2-b]quinoline-3,14(4H,12H)dione} from 10-hydroxycamptothecin. The invention discloses the rationale use of dichloromethane under solid-liquid phase transfer catalysis, which can behave both as solvent and a reactant when it serves as a source for C-1 unit for amino-alkylation of 10-hydroxy-4-(S)camptothecin.
Claims10
A process for preparing 9-[(dimethylamino)-methyl]-10-hydroxycamptothecin(topotecan) of the formula 1 below
- from 10-hydroxy-20-(S)-camptothecin (HCPT) dissolved in an organic solvent, the process comprising ortho-regioselective aminomethylation of HCPT with dimethylamine, using a dihalomethane which behaves both as solvent and a reactant, under solid-liquid phase transfer catalysis along with a solid base catalyst in suspension form, and under stirring and at room temperate, filtering the solid product obtained and washing the obtained solid product, evaporating the solvent and purifying the residue to obtain the desired product.
Dependencies are inferred from the claim text.