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4-(2-halogenated isobutyryl) phenylethanol derivative and preparation method thereof

A technology for halogenating isobutyryl and phenethyl alcohol, applied in the field of 4-phenylethyl alcohol derivatives and preparation thereof, can solve unseen problems and the like, and achieve the effects of low cost, high industrial production and application value, and mild reaction conditions

Pending Publication Date: 2019-08-09
JINGCHU UNIV OF TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] And 4-(2-halogenated isobutyryl) phenethyl alcohol derivatives and synthetic method thereof, do not see relevant bibliographical information

Method used

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  • 4-(2-halogenated isobutyryl) phenylethanol derivative and preparation method thereof
  • 4-(2-halogenated isobutyryl) phenylethanol derivative and preparation method thereof
  • 4-(2-halogenated isobutyryl) phenylethanol derivative and preparation method thereof

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Embodiment Construction

[0028] Preferred examples of the invention will be described in detail below. The examples given are to better explain the content of the invention, and the content of the invention is not limited to the examples. Non-essential improvements and adjustments to the embodiment according to the content of the invention still belong to the scope of the invention.

[0029] (1), Synthesis of 4-(2-chloroisobutyryl) phenylethyl alcohol acetate (2) (Pg=CH 3 CO,X=Cl)

[0030]

[0031] In a 500ml three-neck flask, weigh phenylethyl acetate (20.0g, 0.12mol), add 100ml of dichloromethane and stir, cool down to 0°C, add anhydrous aluminum trichloride (32.0g, 0.24mol) and stir, drop Chloroisobutyryl chloride (19.7 g, 0.14 mol) was added, kept at 0°C for 1 hour, returned to room temperature (25°C) and stirred for 4 hours. After the reaction, dilute hydrochloric acid was added to quench the reaction, dichloromethane was added to extract twice, the organic phases were combined, the organic...

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Abstract

The invention provides a 4-(2-halogenated isobutyryl) phenylethanol derivative. The derivative is characterized in that the structural general formula of the 4-(2-halogenated isobutyryl) phenylethanolderivative is shown in the description, wherein X refers to Cl or Br, and Pg refers to a hydrogen atom or a hydroxyl protective group. The invention also discloses a preparation method of the 4-(2-halogenated isobutyryl) phenylethanol derivative. The preparation method of the 4-(2-halogenated isobutyryl) phenylethanol derivative has the advantages that the cost of raw materials is low, the reaction conditions are mild, and a higher industrial production application value is achieved.

Description

technical field [0001] The invention relates to the field of chemical synthesis, in particular to a 4-(2-halogenated isobutyryl)phenethyl alcohol derivative and a preparation method thereof. Background technique [0002] Bilastine is a second-generation histamine H1 receptor antagonist developed by Spain's FAES Pharmaceutical Company. It was approved by the European Union in 2012 for the treatment of allergic rhinitis and chronic idiopathic urticaria. [0003] [0004] Among them, α,α-dimethyl-4-(hydroxyl-protected hydroxyethyl) phenylacetate derivatives (bilastine intermediate and its analogues) are an intermediate for the synthesis of bilastine, It can be obtained from the 4-(2-halogenated isobutyryl)phenylethanol derivative of the present invention through two-step reaction of ketal and rearrangement. [0005] [0006] And 4-(2-halogenated isobutyryl) phenethyl alcohol derivatives and their synthetic methods, no relevant literature reports. 4-(2-Haloisobutyryl)phe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C67/29C07C69/63C07C303/30C07C309/73
CPCC07C45/64C07C67/29C07C69/63C07C303/30C07C309/73C07C69/157C07C49/82Y02P20/55
Inventor 李立威许方亮
Owner JINGCHU UNIV OF TECH
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