Methyl 2-amino-5-iodothiazole-4-carboxylate synthesis

Yield:1235034-76-0 94%

Reaction Conditions:

with N-iodo-succinimide in dichloromethane at 20; for 24 h;

Steps:

8.1

To a solution of methyl 2-aminothiazole-4-carboxylate (5.6g, 35.4mmol) in DCM (6OmL) was added NIS (9.56g, 42.5mmol). The mixture was stirred at rt for 24 hours and then diluted with EtOAc (20OmL) and washed with water, brine, dried over Na₂SO₄, and concentrated under reduced pressure to provide 9.5 g (94%) of the desired product methyl 2- amino-5-iodothiazole-4-carboxylate (8A): LC/MS(APCI): m/z 284.9 (M+H).

References:

WO2010/80503,2010,A1 Location in patent:Page/Page column 96-97