Process for the production of purines

C - Chemistry – Metallurgy – 07 – D

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C07D 473/00 (2006.01) C07D 473/16 (2006.01) C07D 473/18 (2006.01) C07D 473/34 (2006.01)

Patent

CA 2152722

In order to produce a purine of the general formula (I), Image (I) in which R1 and R2 can be the same or different and denote H, OH, SH, NH2, N-(di)-alkyl, halogen, O-alkyl, S-alkyl, alkyl or aryl and alkyl represents an aliphatic residue with 1 to 4 carbon atoms and aryl represents a phenyl residue which is substituted if desired by CH3, OH, NH2 or halogen, from the corresponding 4-amino-5- nitrosopyrimidine of formula (II), Image (II) in which R1 and R2 have the above-mentioned meaning, the compound of formula (II) is reductively formylated in a solvent at a temperature of 80 to 220°C in the presence of formic acid and a catalyst based on a noble metal and the 4-amino-5-formylaminopyrimidine formed as an intermediate is cyclized.

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