Methanol → Methyl 4-amino-2-(methylsulfonyl)thiazole-5-carboxylate

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Reaction Steps

After adding 45.2 g of 4-amino-2-methylsulfanylthiazole-5-carboxylic acid methyl ester [CAS No. 60093-05-2] to 2 l of a water:methanol=1:1 mixed solvent at room temperature, 408 g of Oxone® was gradually added over a period of 30 minutes while stirring. Stirring was continued for 24 hours at room temperature, and then the reaction mixture was poured into a mixture of 10 l of ethyl acetate and 10 l of water. The organic layer was washed with 5 l of brine and dried over anhydrous magnesium sulfate. The desiccant was filtered out and the filtrate was concentrated under reduced pressure to obtain the target compound (37.6 g) as a colorless solid.

Provenance & Evidence