Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Method for continuously synthesizing cefixime side chain acid active ester

A technology of cefixime side chain acid and active ester, applied in the field of medicine, can solve the problems of long residence time of materials, poor product quality uniformity, poor energy utilization rate, etc., achieve stable heat release, easy temperature control, and reduce VOC The effect of emissions

Pending Publication Date: 2022-01-21
山东普洛得邦医药有限公司 +1
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the deficiencies in the prior art, the intermittent reaction process causes the problems such as long residence time of materials, poor energy utilization rate, and poor product quality uniformity. The invention provides a continuous synthesis method of cefixime side chain acid active ester

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

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Method for continuously synthesizing cefixime side chain acid active ester
  • Method for continuously synthesizing cefixime side chain acid active ester
  • Method for continuously synthesizing cefixime side chain acid active ester

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The side chain acid active ester of cefixime was synthesized by a three-stage serial tank reactor, each reactor had a volume of 5 L, and each reactor was connected in series by a metering pump. In the slurry configuration kettle of 50L, cefixime side chain acid: dithiodibenzothiazole: acetonitrile is added by weight ratio 1:1.4:8.0, starts to stir, presses 200g / min by metering pump, simultaneously catalyst (three The weight ratio of ethylamine: pyridine: dimethylaniline is 1:0.2:0.3) according to the weight ratio of 0.025:1 to the slurry, the catalyst is added through the metering pump at a speed of 5g / min, and then added to the first-stage reaction kettle. According to the weight ratio of triethyl phosphate to the slurry of 0.078:1, add triethyl phosphite through the metering pump at a speed of 15.5g / min, and then add it to the first-stage reaction kettle; The feed liquid of the first-stage reactor is added to the second-stage reactor, and after 40 minutes, the feed li...

Embodiment 2

[0039]The side chain acid active ester of cefixime was synthesized by a three-stage serial tank reactor, each reactor had a volume of 5 L, and each reactor was connected in series by a metering pump. In the slurry configuration kettle of 50L, cefixime side-chain acid: dithiodibenzothiazole: acetonitrile is added by weight ratio 1:1.4:8.0, starts to stir, presses 133g / min by metering pump, simultaneously catalyst (three The weight ratio of ethylamine:pyridine:dimethylaniline is 1:0.2:0.3) according to the weight ratio of the slurry to 0.025:1, the catalyst is added through the metering pump at a speed of 3.3g / min, and added to the first-stage reaction kettle, while According to the weight ratio of triethyl phosphite to the slurry of 0.078:1, add triethyl phosphite through the metering pump at a speed of 10.4g / min, and then add it to the first-stage reaction kettle; The feed liquid of the first-stage reactor is added to the second-stage reactor, and after 60 minutes, the feed li...

Embodiment 3

[0041] The side chain acid active ester of cefixime was synthesized by a three-stage serial tank reactor, each reactor had a volume of 5 L, and each reactor was connected in series by a metering pump. In the slurry configuration kettle of 50L, cefixime side chain acid: dithiodibenzothiazole: acetonitrile is added by weight ratio 1:1.4:8.0, starts to stir, presses 100g / min by metering pump, simultaneously catalyst (three The weight ratio of ethylamine: pyridine: dimethylaniline is 1:0.2:0.3) according to the weight ratio of the slurry to 0.025:1, the catalyst is added through the metering pump at a speed of 2.5g / min, and added to the first-stage reaction kettle, and at the same time According to the weight ratio of triethyl phosphite to the slurry of 0.078:1, add triethyl phosphite through the metering pump at a speed of 7.8g / min, and then add it to the first-stage reaction kettle; The feed liquid of the first-stage reactor is added to the second-stage reactor, and after 60 min...

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 method for continuously synthesizing cefixime side chain acid active ester. The method comprises the following steps: adding slurry of cefixime side chain acid and dithiobenzothiazole, a catalyst and triethyl phosphite into a first-stage reaction kettle of serially connected reaction kettles in proportion, starting stirring, and transferring materials among the serially connected reaction kettles through a metering pump; and controlling the reaction kettles connected in series to keep a certain temperature, enabling the reaction liquid to flow out of the last-stage reaction kettle and then enter a cooling kettle, filtrating the obtained reaction liquid after the reaction is completed to obtain a crude product, and post-processing the crude product to obtain the cefixime side chain acid active ester product. The method has the advantages that cefixime side chain acid active ester synthesis realizes continuous reaction, variable control in the reaction process is more stable, the problems of multiple ectopic control points, poor product quality uniformity and low production efficiency caused by intermittent reaction are solved, the product quality consistency is remarkably improved, and the method is suitable for industrial large-scale production.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a method for continuously preparing a pharmaceutical intermediate cefixime side chain acid active ester. Background technique [0002] Cefixime side chain acid active ester (structure shown in formula 1), chemical name is α-(2-amino-4-thiazole)-α-(2-methoxycarbonylmethoxyimino)-benzothiazole acetate Thioester is a key intermediate in the production of cefixime. Cefixime belongs to the third-generation oral cephalosporin antibiotic, which has a broad antibacterial spectrum, strong antibacterial activity, and is highly stable to β-lactamase. Based on the advantages of broad antibacterial spectrum and high efficacy of this third-generation cephalosporin drug, cefixime has a good market prospect, which increases the demand for its cefixime side chain acid active ester. With the development of the industry, the requirements for drug quality and quality uniformity are getting higher...

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): C07D277/74
CPCC07D277/74
Inventor 江海波胡金盛李宁柴家洋
Owner 山东普洛得邦医药有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com