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Preparation method for Dexiansoprazole

A technology of dexlansoprazole and nitro, which is applied in the field of preparing dexlansoprazole, can solve the problems that sulfone is difficult to remove, and achieve the effects of being beneficial to scale-up production, easy to obtain, and simple to operate

Inactive Publication Date: 2014-03-05
SHANDONG INST OF PHARMA IND
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  • Abstract
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  • Claims
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Problems solved by technology

However, the excess reaction product 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfonyl]benzimidazole (hereinafter referred to as sulfone type) are also prepared, usually the sulfone in the sulfoxide is difficult to remove

Method used

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  • Preparation method for Dexiansoprazole
  • Preparation method for Dexiansoprazole
  • Preparation method for Dexiansoprazole

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Embodiment Construction

[0020] The preparation of 2,3-dimethyl-4-nitropyridine-N-oxide, its structural formula is as follows:

[0021]

[0022] Add 10.7 g (0.1 mol) of 2,3-lutidine, 20 mL of glacial acetic acid, and 16 mL (0.15 mol) of hydrogen peroxide with a mass fraction of 30% into a 250 mL three-necked bottle, and heat to 50 ℃, keep warm for 12 hours, distill out water and acetic acid, add dropwise the mixed acid solution prepared by 30 mL (0.54mol) concentrated sulfuric acid and 28 mL (0.4mol) concentrated nitric acid, drop it for about 30 minutes, react at 120~125℃ for 2 hours, cool to room temperature. Pour into 200 mL of cold water, neutralize to PH10~12 with 5mol / L sodium hydroxide solution, extract with dichloromethane (60mL×3), dry over anhydrous sodium sulfate, filter, and concentrate to obtain a yellow solid, which is washed with acetic acid The ethyl ester was recrystallized to obtain 12.5 g of 2,3-dimethyl-4-nitropyridine-N-oxide. Yield 78.1%.

[0023] The preparation of 2-aceto...

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Abstract

The invention relates to a preparation method for Dexiansoprazole. and especially provides a preparation method for Dexiansoprazole preparation method for Dexiansoprazole obtained through reaction of R-2-[[(4-nitro-3-methyl-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole and 2,2,2-trifluoroethanol in the alkaline condition. Dexiansoprazole with high optical purity can be obtained through the method. The operation processes are simple, the reaction yield is high, and the method is suitable for industrial production.

Description

technical field [0001] The invention relates to a method for preparing dexlansoprazole, in particular to a method for preparing dexlansoprazole by substituting trifluoroethanol. Background technique [0002] Dexlansoprazole is a new drug for gastroesophageal reflux disease that is superior to lansoprazole, and its structural formula is: [0003] . [0004] On January 30, 2009, the U.S. FDA approved the listing of a new drug for the treatment of esophagitis, dexlansoprazole (commonly known as Dexiansoprazole), developed by Takeda Pharmaceutical Company of Japan. The drug is an enantiomer of the proton pump inhibitor lansoprazole and is indicated for the treatment of heartburn and varying degrees of erosive esophagitis associated with non-erosive gastroesophageal reflux disease. [0005] Dexlansoprazole is the first dual-release controlled-release (DDR) proton pump inhibitor on the market. The dosage form on the market is a sustained-release capsule, which can make the dr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
CPCC07D401/12
Inventor 邓玉晓刘宪华张宁姜明俊付丙月
Owner SHANDONG INST OF PHARMA IND
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