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Synthesis method of deuterated amiodarone hydrochloride

A technology of amiodarone hydrochloride and a synthetic method, which is applied in the field of synthesis of deuterated amiodarone hydrochloride, can solve the problems of severe reaction conditions and unsuitability for mass production, and achieve the effect of mild reaction conditions

Pending Publication Date: 2020-10-09
SHENZHEN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, in combination with the above-mentioned synthetic method of amiodarone, when making deuterated amiodarone, the reaction conditions of hydrazine hydrate reduction are severe, which is not suitable for mass production

Method used

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  • Synthesis method of deuterated amiodarone hydrochloride
  • Synthesis method of deuterated amiodarone hydrochloride
  • Synthesis method of deuterated amiodarone hydrochloride

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Embodiment Construction

[0037] The technical scheme in the embodiment will be clearly and completely described below

[0038] The term "room temperature" means 0-50°C; in some embodiments, room temperature means 20-40°C, and in some embodiments, room temperature means 25-35°C.

[0039] The "amount of solvent required for the reaction" used in the present invention is preferably to completely dissolve the reactant, and it can be adaptively changed with different reactants. In some embodiments, the amount of solvent required for the reaction may also be adaptively greater than that required to just dissolve the reactants.

[0040] The "inert reaction solvent" used in the present invention has the usual explanation in the field, and specifically refers to a solvent that is not easy to react with reactants and does not affect the reaction process.

[0041] General Synthesis Process

[0042] In general, the compounds of the present invention can be prepared by the methods described in the present invent...

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Abstract

The invention discloses a synthesis method of deuterated amiodarone hydrochloride, and relates to the technical field of medicine synthesis. According to the method, carbonyl is reduced while benzofuranone is subjected to deuteration, the step is milder than a hydrazine hydrate reduction method, reaction can be carried out at the room temperature under one atmospheric pressure deuterium gas, the reaction yield is as high as 93%, and the deuteration rate is 74%; and then a deuterated product is further synthesized to obtain the deuterated amiodarone hydrochloride, the yield is 78%, and the deuteration rate is 73%. The synthesis method of the deuterated amiodarone hydrochloride provided by the invention is mild, efficient, low in cost and suitable for industrial production.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to a synthesis method of deuterated amiodarone hydrochloride. Background technique [0002] During the 1960s, amiodarone, a benzodihydrofuran compound, was mainly used to treat angina pectoris clinically. Later, it was found that it not only blocked potassium channels, but also had certain blocking effects on sodium and calcium channels. α, β receptors also have non-competitive blockade. In the 1970s, amiodarone was officially used as an antiarrhythmic drug in clinical practice, and it was found that the drug had a very broad-spectrum antiarrhythmic effect. maintenance of sinus rhythm), nodal arrhythmia, ventricular arrhythmia (treatment of life-threatening ventricular premature contraction and ventricular tachycardia and prevention of ventricular tachycardia or ventricular fibrillation) and other arrhythmias have excellent Efficacy. Because of its stable and broad-spectru...

Claims

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Application Information

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IPC IPC(8): C07D307/80C07B59/00
CPCC07D307/80C07B59/002C07B2200/05
Inventor 苏陈良欧伟
Owner SHENZHEN UNIV
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