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N-(5-ForMylthiazol-2-yl)acetaMide synthesis

4synthesis methods
-

Yield:252662-37-6 65%

Reaction Conditions:

with diisopropylamine in dichloromethane at 0 - 20; for 17 h;

Steps:

PREPARATION OF NTERMEDIATE 12

Acetyl choride (6 mL, 84.38 mmol) was added to a solution of 2-amino-5- formylthiazole (10 g, 78 mmol) and diisopropylamine (45 mL, 261.1 mmol) in DCM (100 mL) at 0 °C. The resulting mixture was allowed to warm to rt and further stirred atrt for 17 h. NH4C1 (aq. sat. soltn.) was added and the mixture was extracted with EtOAc. The organic layer was separated, dried over MgSO4, filtered and concentrated in vacuo. The residue thus obtained was purified by flash column chromatography (silica; dry load, EtOAc in DCM 0/100 to 50/50) and the desired fractions were concentrated in vacuo to yield intermediate 12 as yellow solid (8.6 g, 65% yield).

References:

WO2018/109202,2018,A1 Location in patent:Page/Page column 44; 45