Preparation method of ropivacaine hydrochloride

A technology of ropivacaine hydrochloride, volume, applied in the field of chemistry, to achieve the effect of simple steps, high purity and high recovery rate

Inactive Publication Date: 2017-11-07
广州市桐晖药业有限公司
View PDF3 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ropivacaine hydrochloride is the hydrochloride salt of ropivacaine, and the preparation method of ropivacaine hydrochloride sold on the market is difficult to simultaneously take into account high purity and high yield

Method used

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
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] A kind of preparation method of ropivacaine hydrochloride is characterized in that, comprises the steps:

[0021] (1) Preparation of intermediate (I): 10 parts by weight of 2-piperidinecarboxylic acid and 120 parts by volume of toluene and chloroform mixture with a volume ratio of 2:1 are added to the conical flask, stirred evenly, and HCl gas is introduced to pH2 ; Erlenmeyer flask is placed in ultrasonic instrument (ultrasonic instrument power is set to 300W), add the N,N-dimethylformamide of 1.5 parts by volume, drop the toluene of thionyl chloride of 13 parts by weight and 20 parts by volume Mixed solution, after dropping, ultrasonic at 40°C for 1.5h, nitrogen gas for 1.5h; dropwise add 20 weight parts of 2,6-dimethylaniline and 30 volume parts of toluene mixture, 45°C for 1.2h, filter to obtain brown wet product, dried to obtain a gray solid, the solid was added to 240 parts by volume of purified water, and stirred to obtain a reaction solution; 10% NaOH solution w...

Embodiment 2

[0026] A kind of preparation method of ropivacaine hydrochloride is characterized in that, comprises the steps:

[0027] (1) Preparation of intermediate (I): 12 parts by weight of 2-piperidinecarboxylic acid and 160 parts by volume of toluene and chloroform mixture with a volume ratio of 2:1 are added to the conical flask, stirred evenly, and HCl gas is introduced to pH3 ; Erlenmeyer flask is placed in ultrasonic instrument (ultrasonic instrument power is set to 300W), add the N,N-dimethylformamide of 1.6 parts by volume, drop the toluene of thionyl chloride of 14 parts by weight and 20 parts by volume Mixed solution, after dropping, ultrasonic at 45°C for 1h, nitrogen gas for 2h; dropwise add 25 parts by weight of 2,6-dimethylaniline and 40 parts by volume of toluene, ultrasonically at 50°C for 1h, filter to obtain a brown wet product, bake Dry to obtain a gray solid, add the solid to 300 parts by volume of purified water, and stir to dissolve to obtain a reaction solution; a...

Embodiment 3

[0032] The difference between this example and Example 1 is that the volume ratio of toluene to chloroform is 1:1 to obtain ropivacaine hydrochloride fine-quality sample 3. The purity is as high as 99.5%; the recovery rate is 86%;

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

PUM

No PUM Login to view more

Abstract

The invention discloses a preparation method of ropivacaine hydrochloride. The preparation method comprises steps as follows: (1) preparation of an intermediate (I), (2) preparation of an intermediate (II), (3) preparation of a crude product and (4) refining. The preparation method has the advantages as follows: the provided preparation method adopts simple steps and is lower in cost and suitable for industrial production, and prepared ropivacaine hydrochloride has high purity and high recovery rate.

Description

technical field [0001] The invention belongs to the technical field of chemistry, and in particular relates to a preparation method of ropivacaine hydrochloride. Background technique [0002] Ropivacaine (Ropivacaine) is a new type of pure L-body long-acting amide local anesthetic listed by Swedish Astra Pharmaceutical Company in 1996. It has dual effects of analgesia and anesthesia, and is widely used in nerve block anesthesia, local infiltration anesthesia and epidural anesthesia. Anesthesia, especially for postoperative analgesia and obstetric anesthesia. Ropivacaine hydrochloride is the hydrochloride salt of ropivacaine, and the preparation method of ropivacaine hydrochloride currently available on the market is difficult to simultaneously take into account high purity and high yield. Contents of the invention [0003] In order to solve the above-mentioned problems in the prior art, the object of the present invention is to provide a preparation method of ropivacaine ...

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

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/60
CPCC07D211/60
Inventor 张彤丽余梓豪
Owner 广州市桐晖药业有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap