An improved three-step synthesis of N2-alkylated guanines has been developed starting from N2-Boc-protected 2-amino-6-chloropurine which was treated with Boc2O, and the resulting doubly N2,9-protected derivative was subjected to N2-alkylation with alkyl halides, followed by hydrolysis. The advantages of this procedure include short reaction steps, simple operations, and good yields.
Method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK)
The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.
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Paragraph 0061-0062
(2014/10/16)
Synthesis of N2-alkyl(aryl, dialkyl, cycloalkyl)guanines
Novel N2-alkyl(aryl, dialkyl, cycloalkyl)guanines have been synthesized by treating 2-chloro-7-benzylhypoxanthine with amines and debenzylation of the N2-substituted 7-benzylguanine products by means of palladium catalyzed hydrogenat