(2-Methoxybenzyl)hydrazine → benzyl 4-(6-(2-methoxybenzyl)-4-methyl-7-oxo-3-(trifluoromethyl)-6,7-dihydro-1H-pyrazolo[3,4-d]pyridazin-1-yl)piperidine-1-carboxylate

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Reaction Steps

To a stirred solution of 112 (361 mg, 0.796 mmol) in EtOH (3.2 mL) was added (2-Methoxy-benzyl)-hydrazine (242 mg, 1.592 mmol) and the resulting solution was allowed to stir for 1 h at room temperature, and for 2 h at 75° C. The solvent was evaporated, saturated NaHCO3 was added and the mixture extracted with EtOAc. After the usual work-up the residue was purified via Biotage (10% to 60% EtOAc/Hexane; 12M column) to afford 113 (81 mg. 18.3% yield) as white solid. LRMS (ESI): calc. 555.6; found 556.3 (MH)+.

Provenance & Evidence