| 摘要 |
PURPOSE: A process for preparing 3-{2-£4-(6-fluorobenzo£d|isoxazol-3-yl) piperidino|ethyl}-2-methyl-6,7,8,9- tetrahydro-4H-pyrido £1,2-a|pyrimidin-4-one is provided, thereby increasing the preparation yield, preparing no by-product and carrying out the process under mild condition. CONSTITUTION: A process for preparing 3-{2-£4-(6-fluorobenzo£d|isoxazol-3-yl) piperidino|ethyl}-2-methyl-6,7,8,9- tetrahydro-4H-pyrido £1,2-a|pyrimidin-4-one represented by the formula(1) comprises reacting a compound of the formula(10) with a compound of the formula(7) under the condition of reduction reaction, wherein the reduction reaction is carried out by reacting the compound of the formula(7) with the compound of the formula(10) in a solvent in the presence of a reducing agent; the solvent is water, C1-6 alkanol, ether, halogenated carbohydrate, aromatic carbohydrate, a dipolar nonprotonic solvent or a mixed solvent thereof; the reducing agent is selected from zinc, H/Pd(or Pt, Ni), seleno-phenol, NaBH4, NaCNBH3, NaBH(OAc)3, LiAlH4, hydrosilan/Lewis acid, BH3/amine, pentacarbonyliron/alcoholic potassium hydroxide or formic acid; and the reduction temperature is 0 to 25 deg. C.
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