.alpha.-halomethyl derivatives of amino acids

C - Chemistry – Metallurgy – 07 – D

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C07D 233/64 (2006.01) C07D 233/54 (2006.01)

Patent

CA 1120041

M?-884 .alpha.-HALOMETHYL DERIVATIVES OF AMINO ACIDS ABSTRACT OF THE DISCLOSURE Novel halomethyl derivatives of amino acids of the following general structure Image wherein Y is FCH2-, F2CH2-, F3C-, ClCH2- or Cl2CH-; R1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, -NR11R12 wherein each of R11 and R12 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms, Image wherein R5 is hydro- R5 gen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R2 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 Image wherein R? is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; each of R3 and R4 is hydrogen, halogen selected from fluorine, chlorine, bromine and iodine, or a straight or branched lower alkyl of from 1 to 4 carbon atoms and may be the same or differ- ent with the proviso that when both R3 and R4 are halogen R3 and R4 are the same; and pharmaceutically acceptable salts thereof.

304902

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