Tetrahydrofuran → Formate

Participants

Reaction Steps

100 mg (1.00 mmol) of 1-methylpiperazine are added to a solution of 242 mg (0.50 mmol) of 6-(3,5-difluorophenyl)-2-[3-(5-trichloromethyl-1,2,4-oxadiazol-3-yl)benzyl]-2H-pyridazin-3-one in 1 ml of THF, and the mixture is stirred at room temperature for 18 hours. The reaction mixture is evaporated and separated by preparative HPLC, giving 6-(3,5-difluorophenyl)-2-{3-[5-(4-methylpiperazin-1-yl)-1,2,4-oxadiazol-3-yl]benzyl}-2H-pyridazin-3-one (“A20”) formate as colourless oil (ESI 465) and 6-(3,5-difluorophenyl)-2-{3-[5-(4-methylpiperazine-1-carbonyl)-1,2,4-oxadiazol-3-yl]benzyl}-2H-pyridazin-3-one (“A21”) formate as colourless solid (ESI 493);

Provenance & Evidence