Hydrazine hydrate (1:1) → ((2S,3R)-2-(Aminomethyl)-3-methylpiperidin-1-yl)(2-fluoro-6-(pyrimidin-2-yl)phenyl)methanone

Participants

Reaction Steps

A stirred solution of the product of Step 240a (99 mg, 0.216 mmol) and NH2NH2.H2O (43 mg, 0.864 mmol) in MeOH (10 mL) was heated to reflux for 2 h. The reaction mixture was cooled to rt then concentrated under reduced pressure. The resulting residue was purified by flash column chromatography on silica gel eluting with CH2Cl2/MeOH/conc. NH4OH (100:0:0 to 90:9:1) to afford the title compound as a white foam (33 mg, 45%). ESI MS (M+H) 329.

Provenance & Evidence