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Method for preparing nebivolol hydrochloride

A compound, the technology of dichloromethane, applied in the field of preparing nebivolol hydrochloride, can solve the problems of harsh reaction conditions, high cost, and many synthesis steps, and achieve mild reaction conditions, low price, and cheap and easy-to-obtain raw materials Effect

Active Publication Date: 2012-02-08
SICHUAN JISHENGTANG PHARMLS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented technology involves making certain chemical substances by reacting two different starting products together through specific steps that involve adding other molecules called nucleophiles (nucleators) beforehand. These new ingredients help make it easier to produce these desired chemical compositions while reducing environmental concerns associated therewith.

Problems solved by technology

In summary, technical problem addressed in this patents relates to improving methods for making nibebufoquidp rosette or similar drugs like Nebulinopristate without reducing their quality due to impurities such as α-cyclodystrophylic acid residue from starting material.

Method used

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  • Method for preparing nebivolol hydrochloride
  • Method for preparing nebivolol hydrochloride
  • Method for preparing nebivolol hydrochloride

Examples

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Embodiment Construction

[0047] The present invention will be further described below through specific implementation in the form of examples. It should be understood that the preparation methods of the examples of the present invention are only used to illustrate the present invention, rather than limit the present invention, and the simple improvements to the preparation methods of the present invention under the premise of the concept of the present invention all belong to the protection scope of the present invention.

[0048] 1. (R, R)-2-(2',2'-dimethyl-[1,3]-dioxol-4-yl)-6-fluoro-4-chromanone and (S, Preparation of R)-2-(2', 2'-dimethyl-[1,3]-dioxolan-4-yl)-6-fluoro-4-chromanone (formula II)

[0049]

[0050] 1. Preparation of 2-bromo-1-(5-fluoro-2-hydroxyphenyl)ethanone

[0051]

[0052] Add 5-fluoro-2-hydroxyacetophenone (160g, 1.03mol) and copper bromide (500g, 2.24mol) into a 3L three-neck flask, then add ethyl acetate (700mL) and dichloromethane (700mL), and stir The temperature was...

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Abstract

The invention discloses a method for preparing nebivolol hydrochloride. An L-nebivolol hydrochloride with four chiral centers and a D-nebivolol hydrochloride with four chiral centers are obtained through carrying out processes of bromination, a wittig reaction, a reduction reaction, a hydrolysis reaction, a condensation reaction, a chiral inversion reaction, a ring-opening addition reaction, a hydrogenation debenzylation reaction, salt forming and the like on raw materials consisting of a simple achiral compound and a cheap chiral aldehyde with only one chiral center. The process of the invention, which has the advantages of cheap and easily available raw material, mild reaction condition, and no pollution to environment, is suitable for the industrialization production.

Description

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Claims

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Application Information

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Owner SICHUAN JISHENGTANG PHARMLS
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