Process for the preparation of 2,4-diamino-5-(3',4',...

Details Process for the preparation of 2,4-diamino-5-(3',4',... Process for the preparation of 2,4-diamino-5-(3',4',...

C - Chemistry, Metallurgy

07

D

260/262.5

C07D 239/49 (2006.01)

Patent

CA 1174679

A B S T R A C T The invention relates to an improved process for the preparation of 2,4-diamino-5-(3',4',5'-trimethoxy- benzyl)-pyrimidine of the general formula I Image (I) by reacting a compound of the general formula II Image (II) (wherein R is an alkyl group having 1-4 carbon atoms) with guanidine, which comprises preparing the said compound of the general formula II by reacting .alpha.-(3,4,5-trimethoxy- benzal)-.beta.-methoxy-propionitrile of the formula III Image (III) with ethylene glycol monoalkylether of the general formula IV HO-CH2-CH2-OR (IV) (wherein R is as stated above) in the presence of an - 2 - alkali alkoxide at a temperature between 60 °C and 90 °C and reacting the compound of the general formula II thus obtained - if desired without isolation - with guanidine in the presence of an alkanol having 4-8 carbon atoms. The advantage of the process is that it is economical and can be carried out with high yields even on industrial scale and provides a product of high purity. The compound of the formula I obtained ie a known chemotherapeutical drug.

406060

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