Process for the manufacture of dipeptide derivatives

Details Process for the manufacture of dipeptide derivatives Process for the manufacture of dipeptide derivatives

C - Chemistry, Metallurgy

07

K

530/5.08

C07K 5/097 (2006.01)

Patent

CA 1056818

Abstract Dipeptide compounds derived from histidyl-proline, namely acyl derivatives of histidyl prolinamide such as orotyl-L-histidyl-L-prolinamide, L-2-oxo-imidazolidine-4-carbonyl-L-histidyl-L-prolinamide, L-5-oxo- thiomorpholine-3-carbonyl-L-histidyl-L-prolinamide and others (and salts of such compounds with pharmaceutically acceptable acids) can be used as psycho-stimulating or anti-depressive agents, respectively. They may be produced for instance by reacting histidyl prolinamide with appropriate acids in presence of an agent, which is able to split off water or with a functional derivative of such an acid. A further preferred process for the preparation of an orotyl-histidyl-prolinamide consists in hydrogenolytic dehalogenation of a 5-chloro- or 5-bromo-histidyl-prolin amide obtained by acylating histidyl prolinamide with 5-chloro- or 5-bromo orotic acid or a functional derivative thereof.

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