4-Hydrazino-2-methylpyridine → 5-[(2S)-2-[[(1,1-Dimethylethyl)diphenylsilyl]oxy]propyl]-N-[4-fluoro-3-(trifluoromethyl)phenyl]-1-(2-methyl-4-pyridinyl)-1H-1,2,4-triazol-3-amine

Participants

Reaction Conditions

Reaction Steps

Mercury(II) chloride (1.8 g, 6.5 mmol) was added to a stirred solution of intermediate D9 (prepared according to Description 9) (3.8 g, 6.5 mmol) and 4-hydrazino-2-methylpyridine (0.8 g, 6.5 mmol) in DMF (65 mL) at room temperature. The reaction mixture was heated at 80° C. for 140 min. The cooled reaction mixture was poured onto ice and the precipitated product was collected by filtration to give a yellow semi-solid. Yield: 4.2 g of intermediate D14 (101.2%).

Provenance & Evidence