Stable polymorphic form of (E)-N,N-diethyl-2-cyano-3-(3,4-dihydr

Details Stable polymorphic form of (E)-N,N-diethyl-2-cyano-3-(3,4-dihydr Stable polymorphic form of (E)-N,N-diethyl-2-cyano-3-(3,4-dihydr

1990-10-31

1992-08-04

Brust, Joseph Paul

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

558401, A61K 31275, C07C25507

Patent

active

051359502

ABSTRACT:
Stable and crystallographically essentially pure polymorphic form A of (E)-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitro-phenyl)acrylamide may be prepared by crystallizing crude synthesis product from lower aliphatic carboxylic acid such as formic or acetic acid with a catalytic amount of hydrochloric or hydrobromic acid added. The product is a potent inhibitor of catechol-O-methyl-transferase enzyme (COMT).

REFERENCES:
patent: 4963590 (1990-10-01), Backstrom et al.
patent: 4971996 (1990-11-01), Shiraishi et al.

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