Patent ID: 6486320
Filing Date: 2002-11-26
Classification: C07C,C07D

Abstract:
Process for the preparation of camptothecin, or of at least one derivative of formula (I): wherein R1, R2, and R3 each represent an identical or different group chosen from:hydrogen, a hydroxyl group, a halogen atom, chosen from fluorine, chlorine, bromine, or iodine, a linear or branched alkoxy group comprising 1 to 4 carbon atoms, a linear or branched alkylthio group comprising 1 to 4 carbon atoms, a (C1-C4)alkylamino group, optionally substituted by one or more C1-C4 alkyl groups, an aralkyl group, optionally substituted by a C1-C4 alkyl group, wherein said aryl group is optionally a heterocycle with 1 to 3 heteroatoms chosen from oxygen, sulfur, and nitrogen, and an arylcarbonyloxy group, wherein said aryl group is optionally a mono- or polycyclic heterocycle with 1 to 3 heteroatoms chosen from oxygen, sulfur, and nitrogen; comprising condensing a 3-(aminomethyl)quinoline derivative and a 5-hydroxy-5-ethyl-6-oxo-5,6-dihydropyrancarboxylic acid or acid derivative, followed by an ethynylation stage, and optionally by at least one of a hydrolysis stage, a double cyclization stage, a dehydrogenation, and a deprotection/dealkoxycarbonylation.