Benzyl Bromide → 3-(4,6-Diamino-5-benzylpyrimidin-2-yl)-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridine

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Reaction Steps

At 110° C., 200 mg (0.74 mmol) of 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboxamidine from Example 25A, 125 mg (0.8 mmol) of 2-benzylmalonodinitrile (preparable from malonodinitrile and benzyl bromide using a base such as potassium carbonate), 0.68 mg (0.8 mmol) of piperidine and 20 ml of 2-pentanol are stirred for 12 h. After cooling, the solvent is evaporated under reduced pressure and the residue is chromatographed over silica gel. This gives 165 mg (52.2% of theory) of the title compound.

Provenance & Evidence