Corynantheidine compounds and preparation method thereof

A technology for conanine base and compound, which is applied in the field of conanine base compounds and their preparation, and achieves the effects of easy control, good stability and high yield

Inactive Publication Date: 2016-10-12
FUDAN UNIV
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, studies on alkaloids in Uncaria show that these alkaloids have the characteristics of high efficiency and low toxicity, a

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
  • Corynantheidine compounds and preparation method thereof
  • Corynantheidine compounds and preparation method thereof
  • Corynantheidine compounds and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0038] 1: Chemical synthesis and preparation

[0039] All solvents, raw materials and reagents used in the present invention are analytically pure or chemically pure unless otherwise specified; the anhydrous treatment of solvents is carried out according to conventional methods.

[0040] Instruments and methods for product separation and identification: Thin-layer chromatography silica gel GF 254 , column chromatography coarse-pore silica gel (200-300 mesh), all produced by Qingdao Ocean Chemical Factory; TLC was detected by 154nm ultraviolet; NMR was measured by Varian VXR-500 NMR instrument, hydrogen spectrum, carbon spectrum with TMS as internal standard .

[0041] 1.1 Synthesis of 1-ethoxycarbonylmethyl-1,2,3,4-tetrahydrocarboline (Formula 2)

[0042] In a 500ml round-bottomed flask, add 200ml of dichloromethane and 30ml of 3,3-diethoxypropionate ethyl ester in sequence with 8g (50mmol) of tryptamine dissolved in it, then slowly add 12ml of trifluoroacetic acid dropwise ...

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 belongs to the field of medicine and pharmacology, and relates to corynantheidine compounds and a preparation method thereof. The corynantheidine compounds adopt the structures shown in formulas (1) and (2). According to the corynantheidine compounds and the preparation method thereof, tryptamine is adopted as a starting material, and multiple steps of reactions of the Pictet-Spengler reaction, the butyl aluminum lithium hydrogen reduction, the Knoevenagel/hetero-Diels+/-Alder cascade reaction, the hydrogenation reaction and the like are adopted to obtain the corynantheidine analogues with the general formulas (1) and (2). The corynantheidine analogues are the new compounds with direct vascular dilation activity, and have the advantages that the synthetic method is simple and convenient, and easy to control, and the synthesized products are large in yield and high in purity; the prepared products are good in self stability, have a wide modification range, can be used for preparing peripheral vascular dilation type antihypertensive drug candidates, and can be used as potential pharmacological tools.

Description

[0001] This application is application number 201310552303X, filing date 2013-11-07, Invention name: Divisional application of Ke Nanyin base compound and its preparation method technical field [0002] The invention belongs to the field of medicine, and relates to conanin base compounds and a preparation method thereof. The present invention uses tryptamine as a starting material, and through multi-step reactions, synthesizes conanine analogues and derivatives thereof; the preparation method has the advantages of strong operability, simple reaction conditions, easy control, and high product purity; The obtained product has good self-stability, can be used to prepare antihypertensive drug candidates for expanding peripheral blood vessels, and can be used as a potential pharmacological tool. Background technique [0003] Uncaria (Ucaria) is a traditional Chinese medicine for lowering blood pressure. After research, its main antihypertensive component is the alkaloid it conta...

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): C07D471/04C07D471/14A61P9/08A61P9/12
CPCC07D471/04C07D471/14
Inventor 朱依谆鲍光植古险峰朱依纯
Owner FUDAN UNIV
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