US 2003/0114414 A1 · Methods for synthesizing substituted pyrimidines

Abstract

Methods of preparing N3-substituted-4-pyrimidones are disclosed. The methods include combining a 4-pyrimidone and a non-aqueous base, followed by an alkylating agent, for a time sufficient for the pyrimidone and the alkylating agent to react. Methods of preparing an N3-substituted-6-(substituted amino)uracil are also disclosed. The methods include (a) combining an N3-substituted-2-alkoxy-6-amino-4-pyrimidone with an amine compound selected from the group consisting of an amine salt and the corresponding free amine, to form a reaction mixture; and (b) heating the reaction mixture to at least 80° C. for a time sufficient for the N3-substituted-2-alkoxy-6-amino-4-pyrimidone and the amine compound to react to form the final product.

Claims53

Dependent claims

A method of preparing an N3-substituted-4-pyrimidone, the method comprising

(a) contacting a 4-pyrimidone with a non-aqueous base and an alkylating agent that includes an appropriately substituted alkyl moiety and a leaving group to form a reaction mixture;
and
(b) maintaining the reaction mixture for a time sufficient for the 4-pyrimidone to be substituted in the N3-position with the appropriately substituted alkyl moiety.

Dependencies are inferred from the claim text.

Methods for synthesizing substituted pyrimidines

Life of this patent

Methods for synthesizing substituted pyrimidines

Life of this patent

Abstract

Claims53