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Preparation method of non-steroidal anti-inflammatory analgesic lornoxicam

A technology of non-steroidal anti-inflammatory and lornoxicam, which is applied in the field of medicine, can solve the problems of high toxicity and low yield, and achieve the effect of short process route, high purity and novel route

Inactive Publication Date: 2017-06-27
IANGSU COLLEGE OF ENG & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This route uses methyl iodide or dimethyl sulfate, which is highly toxic and has a low yield

Method used

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  • Preparation method of non-steroidal anti-inflammatory analgesic lornoxicam
  • Preparation method of non-steroidal anti-inflammatory analgesic lornoxicam
  • Preparation method of non-steroidal anti-inflammatory analgesic lornoxicam

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specific Embodiment

[0022] The first step: the preparation of 2-N-methyl-2-N-Boc-acetyl (2-pyridyl) amine (I)

[0023] Boc-sarcosine 190kg, dissolved in 800kgTHF, add HOBt 150kg, triethylamine 120kg, add 220kg EDCi in batches at zero degree, after adding, react at room temperature for 2h, after the reaction, add 2-amino The tetrahydrofuran solution of pyridine (110Kg 2-aminopyridine dissolved in 150kgTHF) was added dropwise in 1 hour, and reacted overnight at room temperature. Take out after the reaction section, filter, recover THF from the filtrate under reduced pressure, add 300kg of methanol and 500kg of dilute hydrochloric acid to the residue, heat and reflux for 1 hour, the reaction is complete, recover most of the methanol under reduced pressure, add 1mol / L sodium hydroxide solution dropwise at zero temperature, When the pH was about 9, 500kg of ethyl acetate was extracted, dried over anhydrous magnesium sulfate, filtered, and 200kg of ethyl acetate was recovered from the filtrate under re...

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Abstract

The invention discloses a preparation method of non-steroidal anti-inflammatory analgesic lornoxicam. The preparation method includes the steps of enabling 5-chloro-3-chlorosulfonyl-2-methyl carbonate as a starting material to react with 2-N-methyl-2-N-Boc-acetyl(2-pyridyl)amine, and enabling a reactant to react with tertiary butanol and potassium tert-butoxide to obtain the lornoxicam. The preparation method has the advantages of safety, short synthesis route, high yield and environmental protection, and is suitable for industrialized production.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a preparation method of a non-steroidal anti-inflammatory analgesic lornoxicam. Background technique [0002] Lornoxicam, chemical name 6-chloro-4-hydroxy-2-methyl-N-(2-pyridyl)-2H-thieno[2,3-e]-1,2-thiazine-3 -Formamide-1,1-dioxide, trade name Kesaifeng, molecular weight 371.82, divided into injections, tablets and other dosage forms. Lornoxicam is a non-steroidal anti-inflammatory analgesic drug with strong analgesic and anti-inflammatory effects. It is clinically used for various acute mild to moderate pain and joint pain and inflammation caused by rheumatic diseases. [0003] The synthetic method of lornoxicam mainly contains two kinds at present: [0004] A synthetic scheme is to use 5-chloro-3-chlorosulfonylthiophene-2-methyl carbonate as raw material, react with glycine methyl ester hydrochloride, and then cyclize under alkaline conditions, dimethyl sulfate or methyl...

Claims

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Application Information

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IPC IPC(8): C07D513/04
CPCC07D513/04
Inventor 姚文瑾
Owner IANGSU COLLEGE OF ENG & TECH
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