Process for the preparation of 5-formylaminopyrimidines

Details Process for the preparation of 5-formylaminopyrimidines Process for the preparation of 5-formylaminopyrimidines

C - Chemistry, Metallurgy

07

D

C07D 239/28 (2006.01) C07D 239/50 (2006.01)

Patent

CA 2145022

The present invention provides a process for the preparation of 5-formylaminopyrimidines of the general formula:- Image (I) in which R1, R2 and R3 are the same or different and signify H, OH, SH, NH2, alkylamino, halogen, O-alkyl, S-alkyl or alkyl, as well as aryl, and alkyl is an aliphatic radical containing up to 4 carbon atoms, from the corresponding 5-nitrosopyrimidines of the general formula:- Image in which R1, R2 and R3 have the same meanings as above, wherein the starting compound is subjected to a reductive formylation in the presence of a noble metal catalyst, as well as of formic acid and of a,salt thereof. In this way, with low technical expense, it is possible to prepare 5-formylaminopyrimidines with a yield of up to 98% and with a degree of purity of more than 98%.

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