Ammonium formate → 2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4,5-pyrimidinediamine

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Reaction Steps

6-Chloro-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4,5-pyrimidinediamine (74 mg, 0.20 mmol) from example V was dissolved in MeOH (4 ml), and Pd/C (10%, 20 mg) and ammonium formate (126 mg, 2.00 mmol, 10 equivalents) were added. The mixture was heated under reflux for 2 days and then allowed to cool to room temperature before the catalyst was filtered off. Purification took place by preparative HPLC (column: Cromsil 120 ODS, C-18, 10 μm, 250×30 mm, flow rate 50 ml/min, room temperature, gradient: water acetonitrile at 0 min: 90:10, at 28 min 5:95) afforded the desired product.

Provenance & Evidence