Process for the manufacture of racemic (R,R; S,S) asocainol

Details Process for the manufacture of racemic (R,R; S,S) asocainol Process for the manufacture of racemic (R,R; S,S) asocainol

1985-05-03

1987-03-10

Hollrah, Glennon H.

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

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

C07D22508

Patent

active

046491961

ABSTRACT:
A process for the preparation of racemic asocainol in the (R,R; S,S)-form and (-)-asocainol in the (S,S)-form as well as the pharmacologically compatible salts thereof is herein described on the basis of a thermal rearrangement of the inactive (R,S)-diastereomer to the (S,S)-form.
Racemic (.+-.)-asocainol and the (-)-enantiomer are potent antiarrhythmic agents and local anesthetics.

REFERENCES:
patent: 4415495 (1983-11-01), Satzinger et al.
Journal of the American Chemical Society, 80, Jan. 20, 1958, Easton, Pa. USA; J. A. Berson et al. "Asymmetric Induction Studies with Optically Active Biphenyls, the Reactions of Phenylglyoxylates of the Phenylglyoxylates Series with Methylmagnesium Iodide"; pp. 445-451.

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