Methods for preparing irinotecan

Details Methods for preparing irinotecan Methods for preparing irinotecan

C - Chemistry, Metallurgy

07

D

C07D 491/22 (2006.01)

Patent

CA 2567922

Methods for manufacturing 7-ethyl-10-[4-(1-pipendino)-1-piperidino]- carbonyloxy- camptothecin are described comprising reacting a mixture of 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride and 7-ethyl-10- hydroxycamptothecin in a polar aprotic solvent with a base in the presence of catalytic amounts of a N-containing cyclic organic compound having 3 to 20 carbon atoms and optionally in the presence of a water binding agent in an amount which effectively binds any water present in the above reactants and solvents, or reacting A 7-Ethyl-10-hydroxycamptothecin in a polar aprotic solvent with phosgene, trichlormethyl- chloroformate, bis(trichloromethyl)carbonate or a alternative to phosgene and a base in the presence of catalytic amounts of a N-containing cyclic organic compound having 3 to 20 carbon atoms and subsequently B with piperidinopiperidine and an amine base

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