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Lixivaptan crystal form I and preparation method and use thereof

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: 2014-09-24
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 I and preparation method and use thereof
  • Lixivaptan crystal form I and preparation method and use thereof
  • Lixivaptan crystal form I and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Weigh 20.0g of lixiptan, add 80mL of methanol, heat to 60°C and stir for 1 hour, naturally cool to room temperature, a solid precipitates, filter, and vacuum dry for about 24 hours to obtain white crystals of lixiptan (form I) .

Embodiment 2

[0049] Weigh 20.0g of lixiptan, add 40mL of methanol, heat to 60°C and stir for 2 hours, naturally cool to room temperature, a solid precipitates, filter, and vacuum dry for about 24 hours to obtain white crystals of lixiptan (form I) .

Embodiment 3

[0051] Weigh 20.0g of lixiptan, add 120mL of methanol, heat to 60°C and stir for 3 hours, naturally cool to room temperature, a solid precipitates, filter, and vacuum dry for about 24 hours to obtain white crystals of lixiptan (form I) .

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Abstract

The invention belongs to the field of anti heart failure drugs, and more specifically, relates to lixivaptan crystal form I and a preparation method and use of a pharmaceutical composition containing the lixivaptan crystal form I in preparation of drugs for treating hyponatremia. The lixivaptan crystal form I is prepared from 2-chloro-4-nitro benzoic acid as a starting material by esterification, hydrogenation reduction, acylation, hydrolysis, acyl chlorination and other reaction steps, and the prepared lixivaptan purity is 97.5%. The lixivaptan crystal form I and its powder are characterized by X ray diffraction diagrams, and the lixivaptan crystal form I is important for obtaining of compounds with high purity, very determined crystal form and good reproducibility due to good prospects for development and pharmaceutical value of the lixivaptan crystal form I.

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 I 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 an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61K31/5517A61P3/12A61P1/14A61P9/04A61P5/00
CPCC07D487/04
Inventor 刘登科白玫刘颖穆帅张大帅
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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