Yield:301165-22-0 95%

Reaction Conditions:

with triethylamine in dichloromethane at -5; for 1 h;

Steps:

E1

Preparation of 2-Bromo-2-methyl-N-thiazol-2-yl-propionamide used in Example El is described below. 2-Bromo-2-methyl-N-thiazol-2-yl-propionamide:To a solution of 2-aminothiazole (0.5, 5mmol) and triethyl amine (2.0 ml, 15 mmol) in DCM (10 ml) 2-Bromo-2-methyl-propionyl bromide (0.74 ml, 6 mmol) was added drop wise over a period of 10-15 min at -5⁰C and stirred for 1 h. The reaction mixture was diluted with DCM (25 ml), washed with brine (2X 5 ml), dried over Na₂SO₄. Solvent was evaporated under reduced pressure to yield 2-Bromo-2-methyl-N-thiazol-2-yl-propionamide (1.18 g, 95 %) of product which was used as such for the next step.

References:

WO2008/104994,2008,A2 Location in patent:Page/Page column 46-47