(2-AMino-thiazol-5-yl)-acetic acid Methyl ester hydrobroMide synthesis

Yield:723278-34-0 69%

Reaction Conditions:

in methanol at 20 - 80; for 102 h;

Steps:

1.l

Methyl 3-bromo-4-oxobutanoate (1.07 mol assumed) was added to a suspension of thiourea (73 g, 0.96 mol) in methanol, giving an exotherm. The reaction was heated at 80 °C for 6 hours, cooled and then allowed to stand at ambient temperature for 4 days. The product was collected by suction filtration and washed with methanol to give methyl (2-AMINO-1, 3- thiazol-5-yl) acetate hydrobromide (173 g, 69 % yield) as a yellow crystalline solid: 'H-NMR (DMSO d6): 9.25 (bs, 2H), 7.20 (s, 1H), 3.80 (s, 2H), 3.60 (s, 3H)

References:

WO2004/58752,2004,A1 Location in patent:Page 66