Methyl morpholine oxide → (R)-4-(1-cyclopropylethylamino)-6-(3-(1,2-dihydroxyethyl)phenyl)pyrrolo[1,2-b]-pyridazine-3-carboxamide

Participants

Reaction Conditions

Reaction Steps

To a solution of (R)-4-(1-cyclopropylethylamino)-6-(3-vinylphenyl)pyrrolo[1,2-b]pyridazine-3-carboxamide (54.7 mg, 0.158 mmol) in THF/water (4/1) (Volume: 2 mL) at 0° C. were added 4-methylmorpholine N-oxide (0.082 mL, 0.395 mmol) and osmium tetroxide 4% in water (0.039 mL, 6.32 μmol). The reaction mixture was warmed up to 23° C. and stirred for 16 hrs. The reaction mixture was purified on Preparative HPLC (Method A) to yield the desired product (32.2 mg, 41% yield). MS (ES+) m/z: 381.2 (M+H); HPLC: 100%, retention time: 2.836 min (analytical HPLC Method B).

Provenance & Evidence