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Lixivaptan crystal form II, preparation method and use thereof

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

Active Publication Date: 2014-04-30
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • 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

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  • Lixivaptan crystal form II, preparation method and use thereof
  • Lixivaptan crystal form II, preparation method and use thereof
  • Lixivaptan crystal form II, preparation method and use thereof

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).

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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

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Application Information

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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
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