| 摘要 |
<p>Methods for manufacturing 7-ethyl-10- [4- (1-piperidino)-1-pipendino]-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, trichlormethylchloroformate, 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.</p> |
