1,2-Dichloroethane → 2-[1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpyrimidine-5-carboxamide

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Reaction Steps

Under argon, 250 mg (0.688 mmol) of the compound from example 45A were initially charged in dimethylformamide (3.8 ml). Subsequently, 145 mg (0.757 mmol) of EDC and 116 mg (0.757 mmol) of HOBt were added, and finally 77 μl (1.03 mmol) of aqueous ammonia solution (25%) were added. The reaction mixture was stirred at RT overnight and then diluted with ethyl acetate. The organic phase was washed once each with water and saturated aqueous sodium chloride solution, dried over magnesium sulfate, filtered and concentrated by rotary evaporation. The residue was admixed with tert-butyl methyl ether, and the solids were filtered off and dried under high vacuum. This gave 171 mg (66% of theory) of the title compound in solid form.

Provenance & Evidence