Methods for the synthesis of unsymmetrical cycloalkyl substituted xanthines

A process for preparing a compound of formula VII:

• the process, comprising:
• (a) contacting a 5,6-diamino-1H-pyrimidine-2,4-dione of formula II:
• with an acylating agent of formula VI:
• in an aprotic solvent to produce a 1H-pryimidine-2,4-dione of formula IV:
• (b) contacting the 1H-pryimidine-2,4-dione of formula IV with a base to produce a xanthine of formula VII;
• wherein:
• X′ and X″ are each independently selected from the group consisting of Cl, Br, and I;
• R1 is (C3-8)cycloalkyl;
• and,
• R2 is hydrogen, or is selected from the group consisting of substituted or unsubstituted (C1-8)alkyl, halo(C1-8)alkyl-, (C3-8)alkenyl, (C3-8)alkenyl(C1-8)alkyl-, (C3-8)alkynyl, (C3-8)alkynyl(C1-8)alkyl-, (C1-8)alkoxy, (C3-8)cycloalkyl, (C3-8)cycloalkyl(C1-8)alkyl-, (C4-10)hererocyclyl, (C4-10)heterocyclyl(C1-8)alkyl-, (C6-10)aryl, (C6-10)aryloxy, (C6-10)aryl(C1-8)alkyl-, (C5-10)heteroaryl, and (C5-10)heteroaryl(C1-8)alkyl-.