Acetic Acid → 5-ethyl-6-(2-{4-[2-(4-methyl-piperidin-1-yl)-ethoxy]-phenyl}-benzoxazol-6-yl)-4,5-dihydro-2H-pyridazin-3-one

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Reaction Steps

11 mg (29 μmol) {4-[6-(4-ethyl-6-oxo-1,4,5,6-tetrahydro-pyridazin-3-yl)-benzoxazol-2-yl]-phenoxy}-acetaldehyde are placed in 2 mL DCM and 250 μL DMF. 1.70 μL (29 mmol) acetic acid and 3 μL (42 μmol) 4-methylpiperidine are added and the mixture is stirred for 20 min at RT. Then 9 mg (42 μmol) sodium triacetoxyborohydride are added and the mixture is stirred overnight at RT. The reaction mixture is diluted with DCM and extracted successively with 10% sodium carbonate solution and sat. saline solution. The solv. of the organic phase is eliminated i.V. and the residue is purified through KG. (DCM/MeOH+ammonia) the solv. of the corresponding fractions is eliminated i.V. and the residue is crystallised from EN petroleum ether.

Provenance & Evidence