.alpha.-Halomethyl derivatives of .alpha.-amino acids

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

1984-02-06

1985-12-24

Raymond, Richard L.

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

Organic compounds

Carboxylic acids and salts thereof

2601125R, 560 29, 560 30, 560 39, 560 41, 560159, 560168, 560169, 562448, 562449, 562560, 564153, 564155, 564157, 564164, 564165, 564197, 564198, C07C10124

Patent

active

045607958

ABSTRACT:
Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is F.sub.2 CH--, F.sub.3 C--, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR2## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; each of R.sub.a and R.sub.b can be the same or different and 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 ##STR3## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.1 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 lower alkyl group of from 1 to 4 carbon atoms, or ##STR4## wherein R.sub.3 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 Z is R.sub.a HN(CH.sub.2).sub.n -- and each of R.sub.a and R.sub.b is hydrogen; with the provisos that when Z is .gamma.-guanidinopropyl or .beta.-methylthioethyl, Y is FCH.sub.2 --, F.sub.2 CH-- or F.sub.3 C--; when Z is .gamma.-guanidinopropyl, R.sub.1 is hydroxy; and when Z is .beta.-thioethyl, .beta.-benzylthioethyl, S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl or ##STR5## Y and Y.sub.2 are FCH.sub.2 --, F.sub.2 CH--, or F.sub.3 C-- and are the same, each of R.sub.a and R.sub.b is hydrogen and R.sub.1 is hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof.

REFERENCES:
patent: 4325961 (1982-04-01), Kollonitsch et al.
patent: 4413141 (1983-11-01), Bey et al.

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