.alpha.Acetylene and .alpha.-vinyl derivatives of amino acids

Details .alpha.Acetylene and .alpha.-vinyl derivatives of amino acids .alpha.Acetylene and .alpha.-vinyl derivatives of amino acids

1981-01-16

1982-04-06

Shippen, Michael

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

Organic compounds

Carboxylic acids and salts thereof

544 30, 424177, 424246, 424300, 424314, 424309, 424316, 424319, 424320, 424324, 560 24, 560 34, 560 39, 560 40, 560 41, 560158, 560159, 560168, 560169, 562439, 562445, 562448, 562450, 562560, 564153, 564157, 564159, 564204, 564197, 564198, C07C10352, C07C10128, C07C10368, C07C125065, C07C125073, C07C12912

Patent

active

043237045

ABSTRACT:
Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R.sub.1 is --C.tbd.CH or --CH.dbd.CH.sub.2 ; R.sub.2 is hydrogen or COR wherein R is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.a is hydrogen, ##STR3## 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 ##STR4## wherein R.sub.7 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; and R.sub.b has the same meaning as defined for R.sub.a except R.sub.b is not ##STR5## and R.sub.a and R.sub.b can be the same or different; with the provisos that when R.sub.2 is hydrogen, R.sub.1 is --C.tbd.CH; when A is ethylidene, R.sub.2 is hydrogen; and when R.sub.a is ##STR6## A is methylene; and pharmaceutically acceptable salts and individual optical isomers thereof.

REFERENCES:
patent: 3959356 (1976-05-01), Metcalf
patent: 3960927 (1976-06-01), Metcalf
patent: 4088667 (1978-05-01), Casara
patent: 4133964 (1979-01-01), Metcalf
patent: 4147873 (1979-04-01), Metcalf
patent: 4182891 (1980-01-01), Metcalf
patent: 4260823 (1981-04-01), Casara

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