Argatroban and preparation thereof

A technology of argatroban and a synthesis method, which is applied in the field of drug synthesis, can solve the problems of complicated operation, low yield, large respiratory tract irritation, etc., and achieves the effects of simplified operation steps, simple synthesis process and shortened reaction time.
CN101348481AInactive Publication Date: 2009-01-21TIANJIN TAIPU PHARMA SCI & TECH DEV +1
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
TIANJIN TAIPU PHARMA SCI & TECH DEV
Publication Date
2009-01-21
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a method for synthesizing argatroban. The method comprises the following steps that nitryl L-arginie and quinoline sulfonchloride are condensed, and undergo amidation with piperidine ethyl formate, followed by hydrolysis and hydrogenation to obtain argatroban; the amidation is to make carboxylate (c-v) and (2R, 4R) 4MPE (Z-VII) react in an organic solvent in the presence of condensing agent, or the presence of both condensing agent and dehydration promoter, in which the molecular ratio of carboxylate (c-v): (2R, 4R) 4MPE (Z-VII): condensing agent: dehydration promoter is 1: 0.8-1.2: 0.8-1.2: 0-1.2. The condensing agent adopted by the invention is diphenylphosphoryl azide, diethylthiophosphoryl, chlorophosphoric acid diethyl or bromophosphoric acid diethyl. The invention has simplified operation, lowered cost, decreased pollution, increased yielding rate, and is suitable for large-scale industrialized production of argatroban.
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Description

technical field

[0001] The invention belongs to the technical field of drug synthesis, and relates to a method for preparing chemically synthesized drugs, more specifically, a method for synthesizing argatroban. Background technique

[0002] Stroke is the scientific name of cerebral apoplexy, which is a sudden onset of cerebral blood circulation disorders. The clinical manifestations are mainly characterized by sudden fainting, unconsciousness or sudden crooked mouth and eyes, hemiplegia, strong tongue, and mental retardation. Cerebral stroke includes ischemic stroke (transient ischemic attack, atherosclerotic thrombotic cerebral infarction, lacunar infarction, cerebral embolism), hemorrhagic stroke (cerebral hemorrhage, subarachnoid hemorrhage), high Blood pressure encephalopathy and vascular dementia four categories. According to statistics, there are 2 million stroke patients in my country every year. The incidence rate is as high as 120 / 100,000. There are currently 7...

Claims

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