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

Preparation method of risperidone

A technology for risperidone and piperidinone hydrochloride, which is applied in the field of chemical drug intermediate preparation, can solve the problems of affecting the quality of raw materials, difficult to remove impurities, low total yield and the like, and achieves strong product market competitiveness, The effect of good industrialization and high product yield

Inactive Publication Date: 2019-03-08
浙江工业大学上虞研究院有限公司
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The raw material of this method is easy to get, and it is the mainstream method of risperidone at present, but the total yield is low, and dimer impurities are easily formed in the reaction
This impurity will participate in the follow-up reaction, and the corresponding impurity generated is difficult to remove, seriously affecting the quality of the raw material drug, and repeated recrystallization is required to obtain qualified products

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
  • Preparation method of risperidone
  • Preparation method of risperidone
  • Preparation method of risperidone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Preparation of 2,4-difluorophenyl-4-piperidinemethanone oxime (Ⅲ).

[0023] In a 1000mL airtight four-necked reaction flask, add 52.3 grams of 2,4-difluorophenyl-4,-piperidine ketone hydrochloride (II), 13.9 grams of hydroxylamine hydrochloride, 19.8 grams of N-methylpiperidine and 500mL of ethanol, stirred and controlled the temperature at 60°C, reacted for 12 hours, stopped stirring, cooled to room temperature and filtered to obtain 24.8 grams of white solid 2,4-difluorophenyl-4-piperidinemethanone oxime (Ⅲ), yield 51.6 %.

Embodiment 2

[0024] Example 2: Preparation of 2,4-difluorophenyl-4-piperidinemethanone oxime (Ⅲ).

[0025] In a 1000mL sealed four-necked reaction flask, add 52.3 grams of 2,4-difluorophenyl-4,-piperidine ketone hydrochloride (II), 27.8 grams of hydroxylamine hydrochloride, 19.8 grams of N-methylpiperidine and Ethanol 500mL, stirring temperature control 60 ℃, reacted for 12 hours, stopped stirring, cooled to room temperature and filtered to obtain 36.7 grams of white solid 2,4-difluorophenyl-4,-piperidinemethanone oxime (Ⅲ), yield 76.3%.

Embodiment 3

[0026] Example 3: Preparation of 2,4-difluorophenyl-4-piperidinemethanone oxime (Ⅲ).

[0027] In a 1000mL airtight four-necked reaction flask, add 52.3 grams of 2,4-difluorophenyl-4-piperidine ketone hydrochloride (II), 13.9 grams of hydroxylamine hydrochloride, 39.6 grams of N-methylpiperidine and ethanol 500mL, stirred and controlled the temperature at 60°C, reacted for 12 hours, stopped stirring, cooled to room temperature and filtered to obtain 32.9 grams of white solid 2,4-difluorophenyl-4,-piperidinemethanone oxime (Ⅲ), yield 68.4 %.

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 risperidone, and belongs to the technical field of preparation methods for chemical medical intermediates. High-purity risperidone is prepared by performing oximation, cyclization and condensation reactions on 2,4- difluorophenyl-4,-piperidone methanone hydrochloride and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyridino-[1,2-a]pyridine-4-ketone as raw materials. The method disclosed by the invention has the advantages of adoption of relatively cheap and readily-available raw materials, easiness in operation, higher yield and higher industrial value.

Description

technical field [0001] The invention belongs to the technical field of preparation methods of chemical drug intermediates, and in particular relates to a preparation method of high-purity risperidone. Background technique [0002] Risperidone, whose structure is shown in formula (I), is a benzisoxazole derivative and is a new generation of antipsychotics. It has high affinity with 5-HT2 receptor and dopamine D2 receptor. This product can also bind to α1 receptors, has low affinity to H1 receptors and α2 receptors, and does not bind to cholinergic receptors. This product is a powerful D2 receptor antagonist that can improve the positive symptoms of schizophrenia; but it causes less motor function inhibition and catalepsy than classic antipsychotics. The balance of 5-HT and dopamine antagonism on the central system can reduce the possibility of extrapyramidal side effects and extend its therapeutic effect to the negative symptoms and affective symptoms of schizophrenia. Ora...

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
IPC IPC(8): C07D471/04
CPCC07D471/04
Inventor 方标柯军梁许萌
Owner 浙江工业大学上虞研究院有限公司
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