Preparation method of 2-(4-bromomethyl)phenyl propionic acid

A technology of phenylpropionic acid and bromomethyl, which is applied in the field of preparation of 2-phenylpropionic acid, can solve the problem of high cost and achieve the effects of low toxicity, high purity and simple reaction
CN107501077AInactive Publication Date: 2017-12-22杭州乐敦科技有限公司 +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
杭州乐敦科技有限公司
Publication Date
2017-12-22
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a preparation method of 2-(4-bromomethyl)phenyl propionic acid. The preparation method includes the steps of: performing a reaction to a compound (I) (4-methylstyrene) with hydrogen halide to prepare a compound (II), performing a Grignard reaction and a carboxylation reaction to the compound (II) to obtain a compound (IV), and performing a bromination reaction to obtain a compound (V) (2-(4-bromomethyl)phenyl propionic acid), wherein a byproduct compound (VI) is subjected to a debromination reaction to obtain the compound (V) (2-(4-bromomethyl)phenyl propionic acid). The method is low in cost, has simple operations, is high in yield, is environment-friendly, and is suitable for industrial production.
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Description

technical field

[0001] The invention relates to the technical field of chemical synthesis. Specifically, it relates to a preparation method of 2-(4-bromomethyl)phenylpropionic acid. Background technique

[0002] 2-(4-bromomethyl)phenylpropanoic acid (2-(4-(bromomethyl)phenyl)propanoic acid), with a molecular weight of 243.1, is a key intermediate for the synthesis of loxoprofen sodium. Loxoprofen sodium was first developed by Japan's Sankyo Co., Ltd., and now it is the first-selling variety of non-steroidal anti-inflammatory drugs in Japan. It has been recorded by the Japanese Pharmacopoeia, and China has imported it. This product has been included in the National Ninth Five-Year Plan and one of the recommended trial varieties for new product development in 2010.

[0003] The existing routes for synthesizing 2-(4-bromomethyl)phenylpropionic acid generally have the disadvantages of difficult sources of raw materials, complex production techniques, many by-products, and low ...

Claims

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