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Pyridine methyl sulfinyl imidazopyridine derivative

A methyl and pyridine technology, applied in the field of medicine, can solve the problems of large individual differences in pharmacokinetics, affecting drug efficacy and pharmacokinetic parameters, and slow onset time.

Active Publication Date: 2011-04-27
SHANDONG XUANZHU PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this type of drug has a slow onset time and is not strong enough. It takes several doses (and a few days later) to achieve the maximum acid-suppressing effect, and it may not be able to stably suppress acid for 24 hours. The time of taking the drug and eating may affect the drug. Pharmacokinetic parameters, individual differences in pharmacokinetics, and significant interactions with other drugs

Method used

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  • Pyridine methyl sulfinyl imidazopyridine derivative
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  • Pyridine methyl sulfinyl imidazopyridine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0122] Example 1 Preparation of 2-mercapto-5-methoxy-imidazo[4,5-b]pyridine

[0123] 8.3g (60mmol) of 2,3-diamino-6-methoxypyridine was dropped into the reaction flask, 200ml of 95% ethanol solution was added, and 12.8g (80mmol) of potassium ethoxysulfonate was added, and the mixture was heated at 80°C Heat under reflux for 4 hours, after the reaction is complete, cool to room temperature, pour the reaction solution into 200ml of ice water, stir evenly, adjust the pH to 3-4 with 4N hydrochloric acid, precipitate a solid, filter, wash with water until neutral, and vacuum-dry the filter cake to obtain Product 8.5g, yield: 78.2%.

Embodiment 2

[0124] Example 2 Preparation of 1-(4-chloro-5,6-dimethyl-N-oxypyridin-3-yl)-4-methoxy-2-butanol

[0125] Add 300ml chloroform and 73.1g (0.3mol) 1-(4-chloro-5,6-dimethylpyridin-3-yl)-4-methoxy-2-butanol to the reaction flask, cool to 0 ℃, under stirring, add 96g (0.47mol) 85% m-chloroperoxybenzoic acid in batches, continue to stir for 1 hour, then neutralize with saturated solution of sodium bicarbonate, extract with chloroform (150ml×3), extract with Dry over anhydrous sodium sulfate, filter, and distill off the solvent under reduced pressure to obtain 66.4 g of light yellow solid, yield: 85.2%.

Embodiment 3

[0126] Example 3 Preparation of 2-(2-methoxyethyl)-6,7-dimethyl-2,3-dihydrofuro[3,2-c]pyridine oxide

[0127] Under the protection of nitrogen, add 26.0g (100mmol) of 1-(4-chloro-5,6-dimethyl-N-oxide pyridin-3-yl)-4-methoxy- 2-butanol, 100ml of toluene, then add 4g of 60% NaH (mineral oil), slowly raise the temperature to reflux, keep warm and stir for 2h, evaporate the solvent under reduced pressure, add 100ml of chloroform to the residue, and wash with 1N HCl solution, saturated chlorine respectively After washing with sodium chloride solution, 1N sodium hydroxide solution and deionized water, drying over anhydrous sodium sulfate, and concentration to obtain 16.1 g of the product, yield: 72.1%.

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Abstract

The invention belongs to the technical field of medicine, and in particular relates to pyridinemethylsulfinyl imidazopyridine derivatives shown in a general formula (I), pharmaceutically acceptable salts of the same and isomers of the same, wherein R<1>, R<2>, R<3>, X and Y are defined in a specification. The invention also relates to a method for preparing the compounds, a pharmaceutical composition containing the compounds, and application of the compounds to preparation of medicines for treating peptic ulcer.

Description

1. Technical field [0001] The present invention belongs to the technical field of medicine, and specifically relates to pyridylmethylsulfinyl imidazopyridine derivatives, pharmaceutically acceptable salts and isomers thereof, preparation methods of these compounds, pharmaceutical compositions containing these compounds, and these Application of the compound in preparing medicine for treating and / or preventing peptic ulcer. 2. Background technology [0002] Diseases of the digestive system are one of common frequently-occurring diseases, and the incidence of ulcer disease accounts for about 10% to 12% of the total population. The initial treatment is mainly to use antacids (such as sodium bicarbonate, aluminum hydroxide, etc.) to neutralize gastric acid to relieve symptoms. After the 1970s, with the H 2 The discovery of gastric acid secretion inhibitors such as receptor blockers and proton pump inhibitors has created a new era of peptic ulcer treatment. These drugs have the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D519/00A61K31/437A61P1/04
Inventor 黄振华
Owner SHANDONG XUANZHU PHARMA TECH CO LTD
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