Synthesis and separation identification method for aragatroban related substances

A technology of argatroban and related substances, which is applied in the field of synthesis, separation and identification of related substances of argatroban, can solve the problems that have not been seen in the research reports, and achieve reasonable reaction design, simple and easy operation, and easy operation Effect
CN105273045AInactive Publication Date: 2016-01-27CHONGQING SHENGHUAXI PHARMA CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
CHONGQING SHENGHUAXI PHARMA CO LTD
Publication Date
2016-01-27
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a synthesis and separation identification method for aragatroban two related substances. The method comprises taking aragatroban as a raw material, nitrating by fuming nitric acid, and separating to obtain (2R,4R)-1-[NG-nitro-N2-((R,S)-3-methyl-1,2,3,4-tetrahydro-8- quinolylsulfonyl)-L-arginyl]-4-methyl-2-pipecolinic acid (wherein G in NG and 2 in N2 are both superscripts) (aragatroban related substance A); and taking aragatroban as a raw material, hydrolyzing through an aqueous solution of sodium hydroxide, barium hydroxide or other highly-basic reagent, and separating to obtain (2R,4R)-1-[N-((R,S)-3-methyl-1,2,3,4-tetrahydro-8-quinolylsulfonyl)-L-ornithyl]-4-methyl-2-pipecolinic acid (aragatroban related substance B). The provided preparation method for the aragatroban related substances is simple and practicable, and low in cost, avoids a complex tedious operation process for total synthesis of the aragatroban related substances, and is a suitable preparation method for the aragatroban related substances. The aragatroban related substance A and the aragatroban related substance B are both shown in the specification.
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Description

technical field

[0001] The present invention relates to two argatroban related substances A [(2R, 4R)-1-[N G -Nitro-N 2 -((R,S)-3-methyl-1,2,3,4-tetrahydro-8-quinolinesulfonyl)-L-arginyl]-4-methyl-2-piperidinecarboxylic acid] Argatroban related substance B [(2R,4R)-1-[N-((R,S)-3-methyl-1,2,3,4-tetrahydro-8-quinolinesulfonyl) The synthesis, separation and identification of -L-ornithyl]-4-methyl-2-piperidinecarboxylic acid] belongs to the field of pharmaceutical compound synthesis. Background technique

[0002] Argatroban is a new type of antithrombin active substance researched and developed by Mitsubishi Chemical Corporation of Japan. It is an intravenous injection and has been marketed in many countries with good prospects for clinical application. The chemical name of argatroban is: (2R,4R)-1-[N 2 -((R,S)-3-Methyl-1,2,3,4-tetrahydro-8-quinolinesulfonyl)-L-arginyl]-4-methylpiperidine-2-carboxylic acid- Hydrate. The chemical structural formula is as follows:

[0003] ...

Claims

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