METHOD OF PRODUCING TOPOTECAN Russian patent published in 2012 - IPC C07D491/22 A61K31/47 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing topotecan - a cytostatic agent from a group of camptothecins, which is used as a topoisomerase I inhibitor

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The method involves: a) reducing camptothecin (1) to 1,2,6,7-tetrahydro-20(S)-camptothecin (3) using 2,6-dimethyl-3,5-dicarbmethoxy-1,4-dihydropyridine (2) in the presence of trifluoroacetic acid in chloroform medium at 60°C; b) oxidising 1,2,6,7-tetrahydro-20(S)-camptothecin (3) with iodobenzene diacetate (4) to 10-hydroxy-20(S)-camptothecin (5) in an acetic acid-water medium at 20-25°C; c) obtaining 9-[(dimethylamino)methyl] 10-hydroxy-20(S)-camptothecin (7) reacting 10-hydroxy-20(S)-camptothecin (5) with bis(dimethylamino)methane (6) in acetic acid medium at 20-25°C; d) extracting topotecan - 9-[(dimethylamino)methyl] 10-hydroxy-20(S)-camptothecin hydrochloride via crystallisation from acetone.

EFFECT: invention enables to obtain an end product using a simple method with sufficiently high output.

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