.alpha.-halomethyl derivatives of amines

Details .alpha.-halomethyl derivatives of amines .alpha.-halomethyl derivatives of amines

C - Chemistry, Metallurgy

07

H

260/470, 260/607

C07H 19/16 (2006.01) C07D 209/48 (2006.01)

Patent

CA 1113089

ABSTRACT OF DISCLOSURE Novel halomethyl derivatives of amines of the follow- ing general structure: Image whereTn Y is FCH2-, F2CH- or F9C-; Z is B-methylthioethyl, B-benzylthioethyl, S-(5'-desoxyadenosin-5'-yl)-S-methyl- thioethyl, y-guanidinopropyl, or Image - wherein n 1s 2 or 3 and R1 is hydrogen or lower alkyl of from 1 to 4 carbon atoms wlth the proviso that when R1 is other than hydrogen, n is 2; and each of Ra and Rb is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wheretn the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or Image where7n R2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; with the provisos that when Z is B-benzylthio2thyl or S-(5' desoxyadenosin- 5'-yl)-S-mothylthioethyl, Rb is hydrogen, when Z is B-methylthioethyl, Y is other than FaC-, and when Z is Image - each of Ra and Rb can be the same or different; and pharmaceutically arceptable salts and individual optical isomcrs thereof.

309576

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