Propionamide antitumor agents

Details Propionamide antitumor agents Propionamide antitumor agents

1977-01-21

1978-02-14

Wyman, Daniel E.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

424324, C07C10344, A61K 3116

Patent

active

040738078

ABSTRACT:
The present invention encompasses compounds of the formula ##STR1## AND THE PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF WHEREIN R represents hydrogen or hydroxymethyl. The compounds of the present invention are prepared by condensing N-carbobenzyloxyserine or 2-carbobenzyloxyamino-3-hydroxy-2-hydroxymethylpropionic acid with p- N,N-bis(2-chloroethyl)!phenylenediamine hydrochloride and removing the carbobenzyloxy protecting group by catalytic hydrogenation. These compounds are useful as cytotoxic agents, in particular, antitumor agents.

REFERENCES:
patent: 2876262 (1959-03-01), Ehrhart et al.
patent: 3542850 (1970-11-01), Jansen et al.
Bergel et al., CA 55:2505e (1961).
Safonova et al., CA 60:15978h (1964).
Safonova et al., CA 55:7325i (1961).

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