Method for preparing 4-(4-fluorobenzoyl) butyric acid

A technology of fluorobenzoyl and fluorobenzene, applied in the field of preparation of 4-butyric acid, can solve the problems of high price, high toxicity of fluorobenzene, troublesome handling, etc., and achieves the advantages of low production cost, improved yield and reduced usage. Effect

Active Publication Date: 2014-04-02
ZHEJIANG NHU CO LTD +1
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  • Abstract
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Problems solved by technology

The shortcoming of this method is: the toxicity of fluorobenzene is relatively high, the price is higher, and fluorobenzene is used as a solvent after industrial production, and it is troublesome to deal with, which increases the production cost; and the yield reported in this patent is 79.3%. Only 24% yield in lower repeat

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  • Method for preparing 4-(4-fluorobenzoyl) butyric acid
  • Method for preparing 4-(4-fluorobenzoyl) butyric acid
  • Method for preparing 4-(4-fluorobenzoyl) butyric acid

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Embodiment 1～11

[0033] Treatment of aluminum trichloride: anhydrous aluminum trichloride (purchased from Sinopharm Chemical Reagent Co., Ltd., product number 10000862). Aluminum trichloride was ground into powder in a mortar, sieved with a 40-mesh screen to obtain fine particles of aluminum trichloride, and then the fine particles were baked at 110°C for 1 hour until a large amount of white smoke came out, and then the fine particles were dried under nitrogen protection. Allow to cool down to room temperature.

[0034] Preparation of 4-(4-fluorobenzoyl)butyric acid: under nitrogen protection, add processed aluminum trichloride, fluorobenzene and organic solvent 100mL in a 500mL three-necked bottle according to the raw material ratio in Table 1, mix Stir evenly, put the three-necked bottle under an ice bath, and add glutaric anhydride solution dropwise to it, wherein, the solvent used for the glutaric anhydride solution is the same as that used for dissolving fluorobenzene, and the dosage is 4...

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Abstract

The invention discloses a method for preparing 4-(4-fluorobenzoyl) butyric acid. The method comprises the following steps: with the protection of an inert gas, dispersing fluobenzene and treated aluminum trichloride into an organic solvent to form a dispersion system, subsequently dropwise adding glutaric anhydride into the dispersion system, reacting at 10-30 DEG C after glutaric anhydride is added, and treating after the reaction is completed so as to obtain 4-(4-fluorobenzoyl) butyric acid. By controlling the moisture content and the grain fineness of aluminum trichloride, the conversion rate of the reaction is greatly improved, the production cost is lowered, and high industrial production operability is achieved.

Description

technical field [0001] The invention belongs to the field of synthesis of pharmaceutical intermediates, in particular to a preparation method of 4-(4-fluorobenzoyl)butyric acid. Background technique [0002] Ezetimibe, whose structure is shown in formula (I), is a drug for treating hypercholesterolemia and primary hypercholesterolemia, which was approved for marketing by the US FDA in November 2002. Ezetimibe is a selective cholesterol absorption inhibitor, mainly used to block the exogenous absorption pathway of cholesterol, suitable for the treatment of homozygous familial hypercholesterolemia (HoFH) and homozygous sitosterolemia ( or phytosterolemia). Ezetimibe inhibits the absorption of cholesterol in the intestine by acting on cholesterol transporters, and hardly metabolizes through cytochrome P450 enzymes, with good safety and tolerance. (The Discovery of Ezetimibe: A View from Outside the Receptor, Clader, J.W. Journal of Medicinal Chemistry 2004, 47, 1-9; Synthesis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C59/88C07C51/083
CPCC07C51/083C07C59/88
Inventor 张玉红鞠龙于明段小停
Owner ZHEJIANG NHU CO LTD
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