Hydrochloric Acid → N-(1-phenylethyl)-[6-(4-t-butylphenylsulfonylamino)-2-(4-formylpiperazinyl)-5-(2-methoxyphenoxy)-4-pyrimidinyloxy]-acetamide

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Reaction Steps

N-(1-Phenylethyl)-hydroxyacetamide (50 mg, 0.3 mmol) was dissolved in dimethyl sulfoxide (0.56 ml). Sodium (11.5 mg; 0.5 mmol) was added to the solution, and the resultant mixture was stirred at room temperature for two hours. 4-t-Butyl-N-[6-chloro-2-(4-formylpiperazinyl)-5-(2-methoxyphenoxy)-4-pyrimidinyl]benzenesulfonamide (56 mg; 0.1 mmol) was added thereto, and the resultant mixture was stirred for 1 hour at 120° C., then poured into water, made acidic with hydrochloric acid, and extracted with ethyl acetate. The extracted was washed with water, dried over anhydrous sodium sulfate, and evaporated. The residue was purified by silica gel column chromatography (chloroform:methanol=20:1), to thereby obtain 23.8 mg (yield: 34%) of the title compound as a pale yellow oil.

Provenance & Evidence