US 5,688,947 A · Production of purines via reductive formylation

Abstract

In order to produce a purine of the general formula (I), ##STR1## in which R.sup.1 and R.sup.2 can be the same or different and denote H, OH, SH, NH.sub.2, 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 CH.sub.3, OH, NH.sub.2 or halogen, from the corresponding 4-amino-5-nitrosopyrimidine of formula (II), ##STR2## in which R.sup.1 and R.sup.2 have the above-mentioned meaning, the compound of formula (II) is reductively formylated in a solvent at a temperature of 80.degree. to 220.degree. 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.

Claims25

Dependent claims

Process for the production of a compound of formula (I):

##STR5## wherein R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of H, OH, SH, NH2, N-alkyl, N-dialkyl, halogen, O-alkyl, S-alkyl, alkyl or aryl groups, wherein the alkyl group has from 1 to 4 carbon atoms and the aryl group is a phenyl residue which is non-substituted or substituted by CH.sub.3, OH, NH.sub.2, or halogen;
comprising reductively formylating a corresponding 4-amino-5-nitrosopyrimidine compound of formula (II) ##STR6## wherein R.sub.1 and R.sub.2 comprises the same groups as recited for Formula I in the presence of formic acid and a noble metal catalyst in a solvent at a temperature of from 80.degree. to 220.degree. C. to produce a 40-amino-5-formylaminopyrimidine intermediate and cyclizing said intermediate to obtain the compound of Formula I.

Dependencies are inferred from the claim text.

Production of purines via reductive formylation

Life of this patent

Production of purines via reductive formylation

Life of this patent

Abstract

Claims25