Water → 2-Methyl-2-[(4-{2-[(methylsulfonyl)oxy]ethyl}-1,3-thiazol-2-yl)thio]propionic acid tert-butyl ester

Participants

Reaction Conditions

Reaction Steps

2-{[4-(2-Hydroxyethyl)-1,3-thiazol-2-yl]thio}-2-methylpropionic acid tert-butyl ester (98 g) synthesized in Example 4 and triethylamine (50 mL) were dissolved in dichloromethane (800 mL), methanesulfonyl chloride (38.8 g) was added dropwise under ice-cooling, and the mixture was stirred for 2 hr at 0° C. Water was added to the reaction mixture, and the organic layer was partitioned. The organic layer was washed with saturated brine and dried over anhydrous sodium sulfate, and the solvent was evaporated. The title compound was quantitatively obtained as a crude brown oil and used as it was for the next step.

Provenance & Evidence