Synthesis method of bezafibrate for regulating blood fat

A technology of bezafibrate and synthetic method, which is applied in the field of medicinal chemistry, can solve problems such as difficult purification, many by-products, and long reaction time, and achieve the effects of strong controllability, mild reaction conditions, and high product purity

Inactive Publication Date: 2011-04-27
HEFEI HUAFANG PHARMA SCI & TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The disadvantage of the above-mentioned method is that using p-Hydroxybenzaldehyde and nitromethane is the main raw material, and metals (Zn, Fe, etc.) and metals (Zn, Fe, etc.) and Hydrochloric acid conditions increase the post-treatment difficulty of "three wastes"; in the acylation and condensation steps, phase transfer catalysts and water are used as solvents, the reaction time is long, the process stability is poor, there are many by-products, and it is not easy to purify

Method used

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  • Synthesis method of bezafibrate for regulating blood fat
  • Synthesis method of bezafibrate for regulating blood fat
  • Synthesis method of bezafibrate for regulating blood fat

Examples

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Embodiment 1

[0019] (1) N, O-bis(4-chlorobenzoyl)tyramide

[0020] Take 101.3g (0.58mol) of p-hydroxyphenylethylamine hydrochloride, add 25g of sodium hydroxide and 500ml of anhydrous pyridine into the reaction flask respectively, stir, and add 220g (1.26mol) of p-chlorobenzoyl chloride dropwise at 25°C, After dropping, the temperature was raised to 98-100°C, and the reaction was carried out for 15 minutes. Cool down to 35°C, pour into 2000g of ice-water mixture, acidify to pH 6 with 15% hydrochloric acid, precipitate a white solid, wash with water and 10% sodium bicarbonate successively, and dry to obtain the product N,O-bis(4 -Chlorobenzoyl)tyramide (2) 168.7 g, yield 70.2%, melting point: 200-202°C.

[0021] (2) N-(4-chlorobenzoyl chloride) tyramide

[0022] Take (2) 150g (0.36mol), 1500ml of ethanol, 510ml of 2M potassium hydroxide, heat to 40°C, react for 1 hour, follow the reaction by TLC, after the reaction is completed, cool, add 2M hydrochloric acid to neutralize, water, 10% wa...

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Abstract

The invention relates to the field of medicinal chemistry and discloses a synthesis method of bezafibrate for regulating blood fat. In the synthesis method, stabilized p-hydroxybenzene ethylamine hydrochloride and p-chlorobenzene formyl halide are used as initial raw materials to be substituted, hydrolyzed and condensed to obtain a target compound. The synthesis method has the advantages of low cost, mild reaction conditions, controllable processes and stable quality and is beneficial to industrialized production, the raw materials can be easily obtained and are relatively stabilized, the purity reaches 99.5% by the detection of the high performance liquid chromatography (HPLC), and the total yield is 48.1%.

Description

1. Technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a preparation method of a phenoxyacetic acid blood lipid regulating drug, in particular to a synthesis method of a blood lipid regulating drug-bezafibrate (I). 2. Background technology [0002] Bezafibrate (I) (Bezafibrate) is a second-generation phenoxyacetic acid preparation drug, which can lower blood low-density lipoprotein and cholesterol, and is mainly used for the treatment of type IIb, III, and IV hyperlipidemia. [0003] The synthesis routes of bezafibrate reported in current patents and literature mainly contain the following types: [0004] 1. Operate under water phase conditions, adopt phase transfer catalyst, reduce operating cost (Wu Jie, etc., patent publication number: CN 101353315A). [0005] 2. Use p-hydroxybenzaldehyde and nitromethane as main raw materials, through chemical reactions such as condensation, hydrogenation, acylation, obtain bezafibrate (Zen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C233/73C07C231/12
Inventor 吴宗好廖结海朱仁发
Owner HEFEI HUAFANG PHARMA SCI & TECH
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