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94088-75-2

S-benzothiazol-2-yl 2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)thioacetate synthesis

3synthesis methods
91868-79-0 Synthesis
2-Amino-alpha-(Methoxyimino)-4-Thiazoleacetic  Acid

91868-79-0
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Yield:94088-75-2 97%

Reaction Conditions:

with pyridine;triethylamine;triethyl phosphite in dichloromethane;acetonitrile at 16.5 - 23; for 2 h;Temperature;Reagent/catalyst;

Steps:

1 The green process for synthesizing AE-active ester by microwave assisting comprises the following steps:

Add 30g of aminothiaoximoacidand 50g of DM to 350mL of dichloromethane-acetonitrile mixture at 21-23 °C.Add 7.2mL of triethylamine, 0.4mL of pyridine, cool down to 16.5-18 ° C, add 23mL of triethyl phosphite, add 1h,Using a microwave reactor, the microwave holding temperature was adjusted to 17 ° C, the microwave radiation power was 80 W, the irradiation time was 60 min, and the stirring speed was 100 rpm.Cool down to below 10 ° C, suction filtration to obtain a crude product. The crude product was soaked in 150 mL of methanol at 22-24 ° C for 1 h to obtain 50.8 g of purified AE-active ester.The yield was 97% and the purity was 99.1%.

References:

CN109053628,2018,A Location in patent:Paragraph 0030-0038

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