Method for synthesizing chiral ilaprazole

A synthetic method and chiral technology, which is applied in the field of new process route of optically active ilaprazole, can solve the problem that ilaprazole has no chiral compound, and achieve the effect of novel process, fewer steps and mild reaction conditions
CN108794451AInactive Publication Date: 2018-11-13SHENZHEN HUAXIAN PHARMA TECH CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHENZHEN HUAXIAN PHARMA TECH CO LTD
Publication Date
2018-11-13
Estimated Expiration
Not applicable · inactive patent

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Abstract

Disclosed is a method for synthesizing chiral ilaprazole. The invention belongs to the technical field of pharmacy. At present, reports about ilaprazole chiral compounds are few. The method includes the following steps: under the protection of nitrogen, adding a phase transfer catalyst and isopropyl ether into thioether in order, adding central metal, adding an oxidant, carrying out quenching withan aqueous sodium sulfite solution after reacting at 0 DEG C for 8 hours, carrying out liquid separation, carrying out organic phase desolvation, and then recrystallizing with ethanol to obtain whitecrystals which are the chiral ilaprazole. The method can be used for pharmaceutical research and industrial production of the chiral eprazole. The method has the characteristics of a novel process, few steps, mild reaction conditions and the like.
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Description

Technical field

[0001] The invention belongs to the technical field of pharmacy, and specifically relates to a new process route of optically active ilaprazole. Background technique

[0002] Ilaprazole is a proton pump inhibitor developed and marketed by Livzon Group, with the trade name "Yilian". It belongs to a class 1 new drug and is used to treat duodenal ulcers.

[0003] Other proton pump inhibitor drugs, such as omeprazole, lansoprazole, pantoprazole, and rabeprazole, have corresponding single chiral compounds on the market, namely esomeprazole and dextran Soprazole, levopantoprazole, and dexrabeprazole. However, ilaprazole is currently used in medicine as a racemate, and its single chiral compound has not been reported yet.

[0004]

[0005] When a chiral compound enters a living body, its two enantiomers usually exhibit different biological activities. For chiral drugs, one isomer may be effective, while the other isomer may be ineffective or even harmful. For example, the...

Claims

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