Synthetic method of bilastine intermediate

A synthesis method, the technology of bilastine, applied in the field of synthesis of bilastine intermediates, can solve the problems of difficult industrial operation, large pollution in the synthesis process, long synthesis process, etc., to achieve convenient operation and avoid isomers The effect of too much, too little solvent
CN112778152AActive Publication Date: 2021-05-11湖北英纳氏生物科技有限公司
5 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
湖北英纳氏生物科技有限公司
Publication Date
2021-05-11

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention discloses a synthetic method of a bilastine intermediate, and belongs to the technical field of organic synthesis. The method comprises the steps of (1) carrying out Friedel-Crafts reaction on benzene and alpha-methyl methacrylate in fluoroalcohol A at the temperature of -15 to 25 DEG C to obtain a compound A; (2) carrying out amine ester exchange reaction on the compound A and diisopropylamine at the temperature of 20-50 DEG C to obtain a compound B; and (3) carrying out Friedel-Crafts reaction on the compound B and ethylene oxide in fluoroalcohol B at the temperature of -15 to 25 DEG C to obtain the bilastine intermediate. According to the method, cheap benzene is taken as a raw material, and the intermediate alpha, alpha-dimethyl-4-(2-ethoxyl) phenylacetyldiisopropylamine is obtained through Friedel-Crafts alkylation, amine ester exchange and further Friedel-Crafts alkylation. In the step (2), a diisopropyl group is relatively large, so that the positioning effect is changed, and the problem of excessive isomers in the Friedel-Crafts alkylation process is avoided. The proportion of Friedel-Crafts alkylation para-position and meta-position products can be 95% or above.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention relates to the technical field of organic synthesis, in particular to a method for synthesizing a bilastine intermediate. Background technique

[0002] Bilastine (Bilst for short), the chemical name is 2-[4-(2-{4-[1-(2-ethoxy-ethyl)-1H-benzimidazol-2-yl}B base)-phenyl]2-methyl-propionic acid, cas number 202189-78-4. Bilastine is an oral second-generation histamine H1 receptor antagonist developed by Spanish FAES Pharmaceutical Company. It was registered as a new drug in the European Union in 2009, and was first approved for marketing in the UK and Ireland in 2011, and then successively marketed in Italy, Japan, Canada and other countries. It is used for the treatment of seasonal allergic rhinitis and perennial allergic rhinitis. The dosage specification is 20mg / piece. Other approved indications include pruritus, eczema and hives. This product is safe, without the sedative effect and cardiotoxicity of commonly used antihistamines. ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More