Thioester enantiomeric compounds and their therapeutic uses

Details Thioester enantiomeric compounds and their therapeutic uses Thioester enantiomeric compounds and their therapeutic uses

1993-02-01

1994-03-22

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514867, 558254, A61K 31265, C07C32706

Patent

active

052965090

ABSTRACT:
The (R) or (S) isomer of acetorphan or N-/(acetylthiomethyl)-2-oxo-1-phenyl-3-propyl/(S) alanine methyl ester is prepared by splitting of racemic acetylthio-3-benzyl-2-propanoic acid by reaction with ephedrin, separation of the enantiomeric salt obtained, then freeing of the acid and coupling with the corresponding amino acid ester. The obtained preparations possess remarkable therapeutic activities and can notably be used as drugs.

REFERENCES:
patent: 4513009 (1985-04-01), Rogues et al.
patent: 5208255 (1993-05-01), Duhamel et al.
Greene, T. W. Protective Groups in Organic Synthesis; John Wiley and Sons: New York, 1981; pp. 209-210.
Evans, D. A. et al. J. Org. Chem. 1985, 50, pp. 1830-1835.
Fournie-Zaluski, M.C. et al. J. Med. Chem. 1986, 29(5), pp. 751-757.

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