Selective processes for fosinopril polymorphs

Details Selective processes for fosinopril polymorphs Selective processes for fosinopril polymorphs

1990-02-16

1992-11-10

Berch, Mark L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07F 9572

Patent

active

051625431

ABSTRACT:
Described herein is a process for selectively preparing and interconverting polymorph salts of fosinopril, an antihypertensive agent that inhibits angiotensin converting enzyme. Each polymorph is prepared by mixing an alkali metal carrier, fosinopril, water and a keto and/or hydroxylic solvent and isolating the polymorph formed from the reaction mixture. The less exothermic polymorph A is formed when the water makes up more than about 0.2% of the water and solvents; at about 0.2% or less, the more exothermic polymorph B is formed.

REFERENCES:
patent: 4337201 (1982-06-01), Petrillo, Jr.
patent: 4734508 (1988-03-01), Thottathil
Morris et al., "Investigation of Polymorphism of Fosinopril Sodium . . . " presented at AAPS meeting, Oct. 1989.
Jerewski et al., "Identification and Physico-Chemical Characterization of Fosinopril . . . " presented at AAPS meeting in 1987.

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