GB629471A - Improvements in or relating to the manufacture of a new 2-tertiaryamino pyrimidine - Google Patents

Abstract

2-(N-p-Methoxybenzyl-N-b -dimethylaminoethyl)-aminopyrimidine is manufactured by reacting the sodium derivative of 2-(N-p-methoxybenzyl) - aminopyrimidine with b - dimethylaminoethyl chloride, or the sodium derivative of 2 - (N - b - dimethylaminoethyl) - aminopyrimidine with p - methoxybenzyl chloride, preferably in an inert hydrocarbon solvent. The product is therapeutically useful as an anti-histaminic agent, preferably in the form of its monohydrochloride, which is prepared by treating the base with concentrated hydrochloric acid in the presence of acetone. In an example, 2-(N-p-methoxybenzyl)-amino-pyrimidine is refluxed with sodamide in toluene, and the resulting mixture containing the sodium derivative of the amine is refluxed with b -dimethylaminoethyl chloride. Specification 606,181 is referred to. The Specification as open to inspection under Sect. 91 comprises also the manufacture of other compounds of the general formula <FORM:0629471/IV (b)/1> wherein the pyrimidine ring or the benzene ring, or both, may contain one or more lower alkyl, lower alkoxy or nitro groups as substituents, and wherein R1 and R2 are identical or different lower alkyl radicals (containing up to 6 carbon atoms). In additional examples, b -dimethylaminoethyl chloride is reacted with the sodium derivatives of 2-benzylaminopyrimidine and its 4-methyl and 4 : 6-dimethyl derivatives, and the first product is converted into its hydrochloride. This subject-matter does not appear in the Specification as accepted.