Formic Acid → 3-{1-[6-Chloro-5-(4-methyl-2-oxo-2,3-dihydro-benzoxazole-6-carbonyl)-pyridazin-3-yl]-piperidin-4-yl}-7-methoxy-1,3,4,5-tetrahydro-benzo[d][1,3]diazepin-2-one

Participants

Reaction Steps

360 mg (1.31 mmol) 7-methoxy-3-piperidin-4-yl-1,3,4,5-tetrahydro-1,3-benzodiazepin-2-one, 480 mg (1.19 mmol) 6-(3.6-dichloro-pyridazine-4-carbonyl)-4-methyl-3H-benzoxazol-2-one and 0.300 mL (1.74 mmol) DIPEA were stirred in 3 mL DMF for 4 h at 100° C. Then the reaction mixture was cooled, combined with 0.5 mL formic acid and 15 mL water, the precipitate formed was suction filtered and dried. This was purified by preparative HPLC-MS. The fractions containing the product were combined and freeze-dried.

Provenance & Evidence