CAMPTOTHECIN DERIVATIVES AND PROCESS FOR PREPARING SAME

摘要

S P E C I F I C A T I O N Title: NEW CAMPTOTHECIN DERIVATIVES AND PROCESS FOR PREPARING SAME New camptothecin derivatives, useful as antitumor agents or intermediates therefor, of the general formula (I) <IMG> (I) wherein X is a lower alkyl group, and R is a hydrogen atom or the grouping -COY where Y is a linear or branched unsubstituted C1-C18alkyl group; a lower alkyl group substituted by a halogen atom or a lower alkylthio, amino, acylamino, hydroxyl, lower alkoxy, aryloxy or lower alkoxycarbonyl group; a C3-C19 alkenyl, C3-C19 alkynyl or C3-C8 cycloalkyl group; a C3-C8 cycloalkyl group substituted by an acylamino-lower alkyl group; an N-acylpyrrolidyl group; a phenyl group; a phenyl group substituted by a halogen atom or a trifluoromethyl, nitro, amino, lower alkoxycarbonyl, lower alkyl, phenyl or lower alkoxy; a cinnamyl group; a benzyl group; a naphthyl group; a pyridyl group; a furyl group; or a thienyl group, as well as acid addition salts an? quaternary ammonium salts thereof, and a process for preparing the new camptothecin derivatives by subjecting 7-ethylcamptothecin to the treatment with an N-di-ethylenediamine followed by acylation.