Water → 2-{[4-(2-{[5-(4-Chlorophenyl)pyridin-2-yl]amino}-2-oxoethyl)-1,3-thiazol-2-yl]thio}-2-methylpropionic acid tert-butyl ester

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Reaction Steps

2-[(4-{2-[(5-Bromopyridin-2-yl)amino]ethyl}-1,3-thiazol-2-yl)thio]-2-methylpropionic acid tert-butyl ester (700 mg) obtained in Example 242-2 and 4-chlorophenylboric acid (358 mg) were dissolved in dioxane (8 mL) and 2 mol/L sodium carbonate (4 mL), tetrakis(triphenylphosphine)palladium (88 mg) was added, and the mixture was refluxed for 4 hr. The reaction mixture was cooled, water was added thereto, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure, and the residue was purified by silica gel chromatography (elution solvent; hexane:ethyl acetate=3:2 to 2:1) to give the title compound (450 mg) as a colorless oil.

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