Convergent approach to water soluble camptothecin derivatives

New water soluble camptothecin derivatives with excellent antitumor activity have been designed and synthesized. The synthetic approach includes an efficient route to 7-aminoethyl and 7-aminomethyl camptothecins using either N-Boc protected aminopropion(or aceto)aldehyde or N-methylacetamide as alkylating agents.