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

Oxacyclo-sulfamide spirocyclic medicament template and synthesis method thereof

A technology for the synthesis of cyclic sulfonamide spiro rings, which is applied in the field of synthesis of oxacyclic sulfonamide spiro ring drug templates, can solve the problem of cumbersome methods, selectivity, and lack of feasibility of oxa ring bisamide spiro ring compounds and other problems, to achieve the effect of simple process, few reaction steps and mild conditions

Inactive Publication Date: 2010-10-20
WUXI APPTEC (TIANJIN) CO LTD +1
View PDF8 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method is relatively cumbersome, and there is a problem of selectivity, and it does not have the feasibility of large-scale preparation of 2-substituted oxeterocyclic bisamide spirocyclic compounds

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
  • Oxacyclo-sulfamide spirocyclic medicament template and synthesis method thereof
  • Oxacyclo-sulfamide spirocyclic medicament template and synthesis method thereof
  • Oxacyclo-sulfamide spirocyclic medicament template and synthesis method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

Embodiment 2

Embodiment 3

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 an oxacyclo-sulfamide spirocyclic medicament template and a synthesis method thereof. The method comprises the following steps of: first cyaniding and aminating a tetrahydro-4H-pyran-4-one or tetrahydrofuran ketone compound in a one-pot boiling manner; then reducing a cyanogroup into an amino-group; next directly performing ring closing with amino sulfamide to obtain a 2-N substituted oxacyclo-sulfamide spirocyclic medicament template (a target compound I); and finally easily obtaining a 2,5-N disubstituted oxacyclo-sulfamide spirocyclic medicament template (a target compound II), wherein the compound I and the compound II have the structural formulae. The synthesis method of the invention has the advantages of high efficiency and the large-scale preparation of the oxacyclo-sulfamide spirocyclic medicament templates.

Description

Technical field: the present invention relates to a synthesis method of an oxacyclic sulfonamide spirocyclic drug template. Background technique: As early as the 1970s, spirocyclic compounds were found to have biological activity. After more than 30 years of research and development, a variety of spirocyclic derivatives have been confirmed to have promising therapeutic effects, such as anti-depression, inhibition of angiogenesis (anti-tumor), anti-platelet aggregation (anti-thrombosis), and anti-Algia Merz disease (senile dementia), etc. Oxacyclic sulfonamide spiro ring structure 1 contains hydrogen bond acceptors and donors at the same time, and the presence of hydrogen bond acceptors and donors can increase the chance of interaction between the substrate and the target, thus possibly improving the interaction between the substrate and the protein. The degree of binding to the target can increase the activity of the substrate. Due to the unique structure of this type of...

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): C07D513/10C40B50/08
Inventor 雷建光周凯李亮亮曹亚峰肖贻崧贺海鹰陈曙辉
Owner WUXI APPTEC (TIANJIN) CO LTD
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