Yield:858486-46-1 48%

Reaction Conditions:

with N-Bromosuccinimide in N,N-dimethyl-formamide at 0; for 0.666667 h;

Steps:

D.D.1

Step D.1 : Preparation of the 2-amino-5-bromo-1 ,3-thiazole-4-carboxylic acid:2-aminothiazole-4-carboxylic acid (205 mg) is dissolved in DMF (4,6 ml). NBS (253 mg) is added at 0⁰C. After stirring at 0⁰C for 40 minutes, the DMF is evaporated. The crude solid is triturated in AcOEt and filtered. Another trituration in acetone is performed to give, after filtration and drying, the desired compound 2-amino-5-bromo-1 ,3-thiazole-4-carboxylic acid (yield: 48%).

References:

WO2010/12793,2010,A1 Location in patent:Page/Page column 21