Chloroform → HCID 86705472, compound

Participants

Reaction Steps

To a solution of 46 (270 mg, 0.582 mmol) and EDCI (139 mg, 0.728 mmol) and CHCl3 (10 mL) was added formohydrazide (41.9 mg, 0.698 mmol) and the reaction was stirred at RT for 2 h. Water was added and the mixture was extracted with DCM. The organic layer was separated and concentrated. The crude residue was purified by SiO2 chromatography eluting with a MeOH/DCM gradient (6 to 8% MeOH) to afford 119 mg (36.4%) of N-(1-(4-chloro-3-fluorophenyl)-2-(2-formylhydrazinyl)-2-oxoethyl)-2-(tetrahydro-2H-pyran-4-ylamino)-5,6-dihydropyrido[3,4-d]pyrimidine-7(8H)-carboxamide (48).

Provenance & Evidence