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A kind of synthetic method of istradefylline

A technology of istradefylline and a synthetic method, which is applied in the field of medicine, can solve the problems of reduced yield, low yield, difficulty in simultaneous methylation of dimethyl carbonate, etc., and achieves good reaction selection, high yield, and reduced The effect of hydrolysis

Active Publication Date: 2021-03-12
LIANYUNGANG GUIKE PHARMA
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Problems solved by technology

But obviously, there are competing reactions in the ring closing process, which will significantly reduce the yield. At the same time, it is difficult for the so-called dimethyl carbonate to be methylated at the same time under weakly alkaline conditions, resulting in a significantly lower yield.

Method used

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Experimental program
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Effect test

Embodiment 1

[0017] A synthetic method for istradefylline, comprising the following steps: (1) 1 mass part of compound 1 is dispersed in 5 mass parts of absolute ethanol, heated to 60°C, 1 mass part of anhydrous sodium carbonate is added, and 1.65 parts by mass of compound 2 was dissolved in 5 parts by mass of absolute ethanol, slowly added dropwise for 3 hours, and kept warm for 0.5 hours after the addition; Sodium solution, adjust pH=12, heat to 120°C in airtight, pressure 0.22Mpa, keep warm for 2 hours; (3) After cooling, at 0-5°C, slowly add dimethyl sulfate, compound 1 and dimethyl sulfate Molar ratio of ester = 1:1.05, stirring rapidly for 7 hours; (4) After filtering, heat to 60°C in methanol for beating, filter after cooling, and dry.

[0018] After liquid phase characterization, the final yield was 62.3%, and the purity was 99.7%.

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Abstract

The invention discloses a synthetic method of istradefylline, and belongs to the technical field of medicines. The synthesis method of the istradefylline mainly comprises the steps of acylation, ringclosing, methylation and the like. The method is high in yield, simple in step and single in solvent, wherein reaction selectivity can be effectively promoted and side reactions are reduced; after ring closing is finished, dimethyl sulfate is dropwise added for a methylation reaction by means of the alkalinity of dimethyl sulfate. The method can be more thorough and cleaner than a dimethyl carbonate reaction in the prior art. The whole process can be carried out in one reaction kettle, wherein the solvent only relates to ethanol and subsequently refined methanol and can be recycled, so that the synthesis method has advantages of high reaction selectivity and yield.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a method for synthesizing istradefylline. Background technique [0002] Itradefylline (KW-6002) is an oral adenosine A2a receptor antagonist developed by Kyowa HakkoKirin, a non-dopamine compound, which improves the movement of Parkinson's patients by changing the activity of neurons function, can improve the initial dyskinesia of Parkinson's patients; at the same time, it has brought a turn for the treatment of late Parkinson's patients, and proved that it can affect other neurotransmitters, non-dopamine drugs can benefit late Parkinson's patients; Dopa-like products (L-DOPA) are used in combination for patients with Parkinson's disease to improve the symptoms of diminished efficacy, and can also reduce the dosage of levodopa, thereby preventing or delaying the occurrence of dyskinesia. In order to reduce or avoid the adverse reactions of istradefylline, many researchers at ho...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D473/06
CPCC07D473/06
Inventor 刘志卓长城李响薛旺迁刘子畅
Owner LIANYUNGANG GUIKE PHARMA
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