| 摘要 |
PURPOSE: Provided is a method for preparing (2R, 3R)-4-(4-fluorophenyl)-2-isobutyryl-3-phenyl-4-oxo-N-phenyl-butyramide which is an intermediate the synthesis of atorvastatin under mild condition in high yield. CONSTITUTION: The method comprises the step of reacting the 4-methyl-3-oxo-N-phenylpentamide represented by the formula 3 and the 2-halo-1-(4-fluorophenyl)-2-phenone represented by the formula 4 in the presence of a base and a catalyst to prepare the (2R, 3R)-4-(4-fluorophenyl)-2-isobutyryl-3-phenyl-4-oxo-N-phenyl-butyramide represented by the formula 2a, wherein X is Cl, Br or I. Preferably the base is at least one inorganic base selected from the group consisting of potassium carbonate, calcium carbonate, sodium carbonate, sodium hydride, potassium t-butoxide and potassium methoxide, or at least one organic base selected from the group consisting of triethylamine, diisopropylethylamine and DBU; and the catalyst is NaI or NaBr.
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