Method for preparing important intermediate of tapentadol hydrochloride analgesic

A tapentadol and intermediate technology, applied in the field of drug synthesis, can solve the problems of undesired cost economy and achieve the effect of reducing production cost
CN101948397AInactive Publication Date: 2011-01-19TIANJIN TAIPU PHARMA SCI & TECH DEV
16 Cites 18 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
TIANJIN TAIPU PHARMA SCI & TECH DEV
Publication Date
2011-01-19
Estimated Expiration
Not applicable · inactive patent

Smart Images

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

Abstract

The invention relates to a method for preparing an import intermediate of a tapentadol hydrochloride analgesic, which is (2S)-1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentyl-3-ol hydrochloride. The (2S)-1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentyl-3-ol hydrochloride with optical activity is obtained by the Grignard reaction of a compound II with optical activity and a compound III with optical activity. The Grignard reaction is performed by mixing magneson solution of the compound III and the tetrahydrofuran solution of the compound II at 5 to 10 DEG C and standing the mixed solution at room temperature overnight. The molar ratio of the compound II to the compound III is 0.8-1:1.0-1.5. The preparation method of the invention is not limited by a chiral column split instrument, solves the problem of processing enantiomers as waste chemicals, reduces production cost and is more suitable for large-batch industrial production.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention belongs to the technical field of drug synthesis, and relates to a preparation method of an important intermediate of tapentadol for treating moderate and severe acute pain. More specifically, it is a preparation method of (2S)-1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol hydrochloride. Background technique

[0002] Tapentadol (tapentadolhydrochloride) is a novel oral analgesic drug acting on the central nervous system developed by Johnson & Johnson Company of the United States. Emotional factors inhibit the transmission of pain in the spinal cord, thereby affecting and controlling the activity of the cerebral cortex that perceives pain; the other is the inhibitory effect on the reuptake of norepinephrine, inhibiting its reabsorption into nerve cells, thereby improving brain function. The level of norepinephrine in the blood also plays an analgesic effect. Tapentadol does not rely on metabolic activation and has no metabolic ...

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