Aminoketone derivative and use thereof

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514340, 514342, 514372, 514373, 514378, 514379, 546270, 546275, 546280, 548206, 548207, 548214, 548241, 548248, A61K 31435, C07D21334

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active

054986192

ABSTRACT:
Aminoketone derivative compounds containing a heterocyclic ring bonded to an aminoketone moiety and useful as effective ingredients of centrally acting muscle relaxants and pollakiurea curing agents.
(+)3-phenyl-5-[2-(1-pyrrolidinylmethyl)butyryl]isoxazole, which has a more remarkable central muscle relaxant action as compared with its racemic modification, can be effectively separated from the racemic modification using optically active 10-camphorsulfonic acid as the agent for the optical resolution.

REFERENCES:
Journal of Organic Chemistry, vol. 52, No. 25, Dec. 11, 1987, pp. 5501-5505 US; R. R. Sauers et al, "Synthesis and Phtochemistry of Heterocyclic Norbornenyl Ketones", p. 5504.
Chemical Abstracts, vol. 102, No. 11, Mar. 18, 1985, p. 574, Abstract No. 95628x, Columbus, Ohio, US.
Chemical and Pharmaceutical Bulletin, vol. 34, No. 4, 1986, pp. 1643-1655; T. Tatee et al: "Isoxazole Derivatives as Centrally Acting Muscle Relaxants II. Synthesis and Structure-Activity Relationship of 3-Amino-N-(3-phenyl-5-isoxazolyl)propanamides", p. 1646.
"The Merck Index", 11th Edition, 1989, p. 262, edited by S. Budavari et al Merck & Co., Inc. Rahway, US.
CA 115:114491j Aminoketone . . . thereof. Matsubara et al., p. 901, 1991.
CA 115:207980h Process for . . . -3-phenylisoxazoles. Matsubara et al., p. 1022, 1991.
CA 101:122572n 3-Benzyl- . . . derivatives. Plazzi et al., p. 18, 1984.

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