Targeted cytotoxic anthracycline analogs

Details Targeted cytotoxic anthracycline analogs Targeted cytotoxic anthracycline analogs

C - Chemistry, Metallurgy

07

B

C07B 43/00 (2006.01) C07H 15/252 (2006.01)

Patent

CA 2471775

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.

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