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Related substance of tirofiban hydrochloride as well as preparation and detection method of related substance

A related substance, tirofiban technology, applied in the field of drug synthesis

Active Publication Date: 2021-05-18
WISDOM PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there are few literature reports on related substances of tirofiban hydrochloride in foreign countries, and rare reports in China

Method used

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  • Related substance of tirofiban hydrochloride as well as preparation and detection method of related substance
  • Related substance of tirofiban hydrochloride as well as preparation and detection method of related substance
  • Related substance of tirofiban hydrochloride as well as preparation and detection method of related substance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0025] 1. N-(n-butylsulfonyl)-[4-(4-pyridyl) butyl]-O-[4-(4-pyridyl) butyl]-L-tyrosine ethyl ester (formula 3 )Synthesis

[0026] Weigh 15.0g of compound formula 1, add 200mL of tetrahydrofuran into it, add 35.8g of triphenylphosphine, stir evenly, add 20.6g of compound formula 2, then cool the system down to 0°C, slowly add 35.0g of azodicarboxylic acid bis Ethyl ester, after the dropwise addition, the temperature of the system was raised to 25°C, and the reaction was stirred for 12 hours, and the reaction was complete as detected by TLC. After the solvent was removed from the system under reduced pressure, the residue was purified by column chromatography (heptane:ethyl acetate=3:1), and the collected product points were concentrated to dryness to obtain compound formula 3 (19.5 g, oil).

[0027] 2.N-(n-butylsulfonyl)-[4-(4-pyridyl)butyl]-O-[4-(4-pyridyl)butyl]-L-tyrosine (Formula 4) synthesis

[0028] Weigh 19g of compound formula 3, measure 50mL of tetrahydrofuran, add ...

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Abstract

The invention provides a method for preparing related substances of raw material medicine tirofiban hydrochloride. The related substance is never reported by other literature documents. The synthesis and research of the related substance are beneficial to improving the quality and medication safety of the bulk drug tirofiban hydrochloride.

Description

technical field [0001] The invention relates to related substances of tirofiban hydrochloride and methods for its preparation and detection, and belongs to the field of drug synthesis. Background technique [0002] Tirofiban Hydrochloride (Tirofiban Hydrochloride, chemical name N-(n-butylsulfonyl)-O-[4-(4-piperidinyl)butyl]-L-tyrosine hydrochloride monohydrate) It is suitable for patients with unstable angina or non-Q wave myocardial infarction. The structural formula of tirofiban hydrochloride is as follows: [0003] [0004] Tirofiban, whose International Nonproprietary Drug Name is Tirofiban (trade name Aggrastat), is an antiplatelet drug. It belongs to a class of antiplatelet drugs called glycoprotein IIb / IIIa inhibitors. Tirofiban is the first drug candidate whose origin can be traced to a pharmacodynamic-based virtual screening. Tirofiban is a nonpeptide reversible antagonist of the platelet protein IIb / IIIa receptor, the major platelet surface receptor involved...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G01N1/28G01N24/08G01N30/02
CPCG01N1/28G01N24/08G01N30/02
Inventor 李冰健邱小龙徐涛左智伟刘文博储玲玲胡林邹平
Owner WISDOM PHARM CO LTD
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