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Method for preparing sodium rabeprazole

A technology of rabeprazole sodium and sodium ions, which is applied in the field of preparing rabeprazole sodium, can solve problems such as hindering the production rate of rabeprazole sodium, and achieve the effect of increasing the production rate

Active Publication Date: 2011-10-19
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, after a large number of experimental studies, the researchers found that the "A solvent" and "preferably 20-40°C" described in this method are a kind of technical bias, which hinders the further improvement of the yield of rabeprazole sodium

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Dissolve NaOH (3.34 g, 0.0835 mol) in 300 ml of acetone, add rabeprazole (30 g, 0.0835 mol, purchased from Wuhan Hezhong Biochemical Company) under stirring conditions, stir and react at 52 °C for 2 hours, add 1 g of activated carbon Decolorize for 0.5 hours, filter with suction, add 200ml of n-hexane, stir and react at 52°C for 2 hours, filter with suction, wash the filter cake with an appropriate amount of n-hexane, and dry to obtain 31.8g of off-white powder with a yield of 99.5% and a purity of 99.9%.

[0022] 1 HNMR (CDCL 3 )δ: 1.99(t, 2H, CH 3 OCH 2 CH 2 CH 2 O), 3.25(s, 3H, CH 3 OCH 2 CH 2 CH 2 O), 3.49(t, 2H, CH 3 o CH 2 CH 2 CH 2 O), 2.17(s, 3H, CH 3 ).

Embodiment 2

[0024] Dissolve NaOH (3.34g, 0.0835mol) in 300ml of acetone, add rabeprazole (30g, 0.0835mol, purchased from Wuhan Hezhong Biochemical Company) under stirring conditions, stir and react at 50°C for 2 hours, add 1g of activated carbon Decolorize for 0.5 hours, filter with suction, add 200ml of n-hexane, stir and react at 50°C for 2 hours, filter with suction, wash the filter cake with an appropriate amount of n-hexane, and dry to obtain 31.6g of off-white powder with a yield of 98.9% and a purity of 99.5%.

[0025] 1 HNMR (CDCL 3 )δ: 1.99(t, 2H, CH 3 OCH 2 CH 2 CH 2 O), 3.25(s, 3H, CH 3 OCH 2 CH 2 CH 2 O), 3.49(t, 2H, CH 3 OCH 3 CH 2 CH 2 O), 2.17(s, 3H, CH 3 ).

Embodiment 3

[0027] Dissolve NaOH (3.34g, 0.0835mol) in 300ml of acetone, add rabeprazole (30g, 0.0835mol, purchased from Wuhan Hezhong Biochemical Co., Ltd.) under stirring conditions, stir and react at 55°C for 2 hours, add 1g of activated carbon Decolorize for 0.5 hours, filter with suction, add 200ml of n-hexane, stir and react at 55°C for 2 hours, filter with suction, wash the filter cake with an appropriate amount of n-hexane, and dry to obtain 31.4g of off-white powder with a yield of 98.3% and a purity of 99.5%.

[0028] 1 HNMR (CDCL 3 )δ: 1.99(t, 2H, CH 3 OCH 2 CH 2 CH 2 O), 3.25(s, 3H, CH 3 OCH 2 CH 2 CH 2 O), 3.49(t, 2H, CH 3 OCH 2 CH 2 CH 2 O), 2.17(s, 3H, CH 3 ).

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PUM

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Abstract

The invention relates to a method for preparing sodium rabeprazole. The method is not subjected to concentration, extraction or lyophilization and comprises the steps of reacting rabeprazole with alkaline substances containing sodium ions at 50-55 DEG C and then adding an alkane solvent, thus dissolving out solid sodium rabeprazole.

Description

technical field [0001] The invention relates to a method for preparing rabeprazole sodium, especially a method for preparing rabeprazole sodium at a specific temperature and a specific solvent. Background technique [0002] h 2 Receptor antagonists and proton pump inhibitors are the two most commonly used drugs for the treatment of gastric acid-related digestive diseases. They both increase gastric pH, but proton pump inhibitors act on H+ / K+-ATPase and strongly inhibit gastric acid secretion. And make gastric pH produce larger and lasting rise. Rabeprazole sodium is a new type of proton pump inhibitor, which can be used in the treatment of gastric acid-related diseases, such as peptic ulcer, gastroesophageal reflux disease, Zoller's syndrome and so on. Compared with omeprazole, rabeprazole sodium has a stronger inhibitory effect on H+ / K+-ATPase, and the inhibition can be restored; it has less effect on plasma gastrin levels; it has selective and strong inhibition of Helico...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
Inventor 钟慧娟吕爱锋杨宝海万中晖
Owner JIANGSU HANSOH PHARMA CO LTD
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