New camptothecin derivatives and process for their preparation.

摘要

New camptothecin derivatives of the general formula: <CHEM> wherein R<1> and R<2> each stands for a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aralkyl group or a substituted or unsubstituted aryl group and R<1> and R<2>, taken together with the nitrogen atom to which they are attached, may form a cyclic group. These new derivatives are useful intermediates for preparing pharmaceuticals or other classes of new camptothecin derivatives. These present new derivatives are prepared by treating camptothecin-7-carboxylic acid first with a carboxyl group-activating reagent and then with ammonia or the corresponding amine.