Citric Acid → Ethyl 4-({2-[(5-cyanopyridin-2-yl)amino]ethyl}amino)-6-(2,4-dichlorophenyl)pyrazolo[1,5-a]pyrazine-2-carboxylate

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Reaction Conditions

Reaction Steps

1 g (5 mmol) of ethyl 4-chloro-6-(2,4-dichlorophenyl)pyrazolo[1,5-a]pyrazine-2-carboxylate (Example 12A) was initially charged in 15 ml of dry DMSO, and 1.55 g (4.22 mmol) of 6-[(2-aminoethyl)amino]nicotinonitrile dihydrochloride (Example 2A) and 5.8 ml (33.5 mmol) of N,N-diisopropylethylamine were added and the mixture was heated in a microwave at 150° C. for 30 min. Ethyl acetate and 10% strength citric acid were added, and the reaction mixture was extracted. The organic phase was washed with sodium chloride solution and dried over magnesium sulfate. This gave, after concentration, 1.4 g (70% of theory) of the product as a solid.

Provenance & Evidence