C-(3-METHYL-ISOXAZOL-5-YL)-METHYLAMINE HYDROCHLORIDE synthesis

Yield:-

Reaction Conditions:

with triethylamine in dichloromethane at 0 - 20; for 72.4167 h;

Steps:

1

l-(3-methylisoxazol-5-yl)methanamine hydrochloride (770mg, 5.18 mmol, 1-6), i-tert- butyl dicarbonate (1.13 g, 5.18 mmol), and triethylamine (795 uL, 5.7 mmol) were stirred in DCM (15 mL) at O⁰C for 5 minutes, warmed to room temperature and stirred for 20 minutes more. The reaction was placed in the freezer for 72 hours. The reaction was diluted with EtOAc, washed with water, saturated sodium bicarbonate and brine. The combined organics were dried over Na₂SO₄ and concentrated in vacuo to give the titled compound (1-7). ESI+ MS: 213[MH]⁺.

References:

WO2007/61763,2007,A2 Location in patent:Page/Page column 33