.alpha.-Acetylenic derivatives of .alpha.-amino acids

Details .alpha.-Acetylenic derivatives of .alpha.-amino acids .alpha.-Acetylenic derivatives of .alpha.-amino acids

1977-07-01

1979-01-09

Thomas, Jr., James O.

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

Organic compounds

Carboxylic acids and salts thereof

546243, 546221, 2601125R, 26032645, 2604482N, 260561A, 560157, 560159, 560169, 560171, 562561, 562563, 544 19, 544 30, 424246, 424313, 424319, 424320, C07C10120, C07C10122, A61K 31225

Patent

active

041339649

ABSTRACT:
Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein n is an integer of from 1 to 3; R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; each R.sub.1 is the same and is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.3 R.sub.4 wherein each of R.sub.3 and R.sub.4 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms and can be the same or different, of ##STR3## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and the lactams thereof when n is 2 or 3; and pharmaceutically acceptable salts and individual optical isomers thereof.

REFERENCES:
patent: 2658912 (1953-11-01), Pfister
patent: 2831883 (1958-04-01), Hill
patent: 2873294 (1959-02-01), Kline
patent: 3855271 (1974-12-01), Dillard
patent: 3927047 (1975-12-01), Ichikawa
patent: 3979449 (1976-09-01), Hirsbrunner

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