Preparation of amine derivatives

Details Preparation of amine derivatives Preparation of amine derivatives

C - Chemistry, Metallurgy

07

D

260/606.8

C07D 307/38 (2006.01)

Patent

CA 1256454

A B S T R A C T PREPARATION of Amine Derivatives Compounds of formula (II) Image (II) in which R1 is C1-4 alkyl, preferably methyl, are prepared by reaction of a compound of formula (I) Image (I) where Q is hydrogen or a cation derived from a suitable base with a suitable alkylating agent such as an alkyl halide or a dialkyl sulphate. The compound of formula (II) may be converted into a histamine H2-antagonist containing an -NHC(=CHNO2)NHCH3 end group, e.g. ranitidine by reaction with an appropriate amine. The compound of formula (I) may be prepared by reaction of methyl isothiocyanate with the carbanion of nitromethane (preferably generated in situ by reaction of nitromethane with a suitable base) in the presence of dimethyl sulphoxide as solvent, Q representing the cation derived from the base used to produce the carbanion of nitromethane.

484041

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