Unlock instant, AI-driven research and patent intelligence for your innovation.

Lixiptan crystal form Ⅱ and its preparation method and use

A technology of tanned crystal form and crystal form, applied in the field of anti-heart failure drugs, can solve the problems of high price, low utilization rate and high production cost

Active Publication Date: 2015-11-18
TIANJIN INSTITUTE OF PHARMA RESEARCH
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because raw material 2 is expensive, route 1 takes 2 as starting material, and after multi-step reaction, its utilization rate is low, and production cost is higher

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
  • Lixiptan crystal form Ⅱ and its preparation method and use
  • Lixiptan crystal form Ⅱ and its preparation method and use
  • Lixiptan crystal form Ⅱ and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Weigh 20.0g of lixiptan, add 140mL of dichloromethane-acetone (1:1), heat to 40°C and stir to dissolve, naturally cool to room temperature, a solid precipitates, filters, and dries to obtain white crystals of lixiptan ( crystal form II).

Embodiment 2

[0050] Weigh 20.0g of lixiptan, add 120mL of dichloromethane-acetone (1:1), heat to 40°C and stir to dissolve, naturally cool to room temperature, precipitate a solid, filter, and dry to obtain white crystals of lixiptan ( crystal form II).

Embodiment 3

[0052] Weigh 20.0g of lixiptan, add 140mL of dichloromethane-acetone (1:1), heat to 40°C and stir to dissolve, naturally cool to room temperature, a solid precipitates, filters, and dries to obtain white crystals of lixiptan ( crystal form II).

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 anti-heart failure drugs, and more particularly relates to a lixivaptan crystal form II and a preparation method thereof, a drug composition containing the lixivaptan crystal form II, and a use of the lixivaptan crystal form II in preparation of hyponatremia treatment drugs. According to the present invention, 2-chloro-4-nitrobenzoic acid is adopted as a starting raw material, and esterification, hydrogenation reduction, acylation, hydrolysis, chlorination and other reaction steps are performed to prepare the lixivaptan crystal form II, wherein the purity of the obtained lixivaptan is 97.5%, and the lixivaptan crystal form II is characterized by the powder X-ray diffraction pattern; and due to the good development prospects and the pharmaceutical values of the compound, it is important to obtain the compound with characteristics of high purity, determined crystal form and good reproducibility.

Description

technical field [0001] The present invention belongs to the field of anti-heart failure drugs, and more specifically relates to lixivaptan or N-[3-chloro-4-(10,11-dihydro-5H-pyrrolo) of formula (I) Crystal Form II of [2,1-c][1,4]benzodiazepine-10-ylcarbonyl)phenyl]-5-fluoro-2-methylbenzamide and its preparation method and containing it A pharmaceutical composition and its use in the manufacture of medicines for treating hyponatremia. Background technique [0002] Arginine vasopressin (AVP), also known as vasopressin and antidiuretic hormone, is a nine-peptide cyclic hormone produced by the hypothalamus and released by the pituitary gland. Diuretic, constrict blood vessels, enhance memory, participate in body temperature and immune regulation, participate in social behavior regulation and other different physiological effects. AVP receptors belong to G-protein-coupled receptors, which are divided into three subtypes according to different transmission mechanisms: Vla, Vlb a...

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 Patents(China)
IPC IPC(8): C07D487/04A61K31/5517A61P7/10
CPCC07D487/04
Inventor 刘登科刘颖白玫穆帅张大帅
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
PatSnap Eureka logo

PatSnap Eureka turns technology decisions into work you can execute. Powered by our Innovation Knowledge Graph, it runs expert workflows across engineering, life sciences, materials and intellectual property. Get your review-ready output in minutes.

X (Twitter)LinkedInYouTubeSubstack

© 2026 PatSnap. All rights reserved. 

Terms of Service

 | 

Privacy policy

 | 

Modern Slavery Act Transparency Statement