TARGETED CYTOTOXIC ANTHRACYCLINE ANALOGS

摘要

Disclosed is a process for the conversion of the nitrogen of a primary amino group of an .alpha., .beta. or .alpha., .gamma. hydroxy primary amine into the nitrogen of a monounsaturated nitrogen-containing heterocyclic compound having 5 or 6 atoms in the ring which comprises the sequential steps of: a) treating said hydroxy amine with an excess of a haloaldehyde, wherein the haloaldehyde has the formula: (see formula I) wherein: n=2 or 3; Y is CH2, OCH2, or CH2--CH2; and X is a halogen; b) adding an excess, relative to the hydroxy amine, of an organic base, c) neutralizing the said base with a weak acid; and d) treating with a dilute aqueous acid.