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Salt of sulfinylbenzimidazole compound, and crystal and amorphous form thereof

A technology of sulfinyl and benzimidazole, which is applied in the field of salts of sulfinyl benzimidazole compounds, their crystals and amorphous substances, and can solve undisclosed problems

Inactive Publication Date: 2011-06-29
EISIA R&D MANAGEMENT CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Therefore, 2-[({4-[(2,2-dimethyl-1,3-dioxan-5-yl)methoxy]-3,5-lutidine has not been disclosed -2-yl}methyl)sulfinyl]-1H-benzimidazole salt and its crystal form

Method used

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  • Salt of sulfinylbenzimidazole compound, and crystal and amorphous form thereof
  • Salt of sulfinylbenzimidazole compound, and crystal and amorphous form thereof
  • Salt of sulfinylbenzimidazole compound, and crystal and amorphous form thereof

Examples

Experimental program
Comparison scheme
Effect test

manufacture example 1

[0298] (Production Example 1) (2,2-Dimethyl-1,3-dioxan-5-yl)methanol

[0299]

[0300] A mixture of 2-(hydroxymethyl)-1,3-propanediol (4.09g, 38.5mmol), acetone (130ml, 1768mmol), and 70% perchloric acid (1.37g, 9.55mmol) was stirred at room temperature for 21 hours . After the reaction mixture was adjusted to pH=9 with concentrated aqueous ammonia, it was concentrated. The residue was purified by silica gel column chromatography (silica gel: 100 g, elution solvent: heptane, heptane / ethyl acetate = 1 / 3) to obtain the title compound (4.83 g, yield: 85.8%) as a colorless oil. .

[0301] 1 H NMR (400MHz, DMSO-d 6 )δppm; 1.29 (3H, s), 1.30 (3H, s), 1.64-1.74 (1H, m), 3.35-3.41 (2H, m), 3.61 (2H, dd, J=7, 12Hz), 3.82 ( 2H,dd,J=4,12Hz), 4.54(1H,t,J=5Hz).

manufacture example 2

[0302] (Production Example 2) 2,3,5-collidine 1-oxide

[0303]

[0304] To acetic acid (1.43 kg, 23.83 mol) was added 2,3,5-collidine (1.43 kg, 11.80 mol) over 15 minutes. After 15 minutes, 35% hydrogen peroxide water (1.38 kg, 14.2 mol) was added dropwise over 30 minutes, followed by stirring overnight at 90°C to 95°C. Sodium sulfite (220 g) was added to the reaction liquid. The reaction mixture was poured into a mixture of sodium carbonate (2.5 kg) and water (12 L), and extracted with chloroform (3.0 L×4). The resulting organic layer was concentrated until crystals precipitated, and n-hexane (2.5 L) was added to the precipitate, followed by stirring overnight under ice-cooling. The obtained crystals were filtered to obtain 1.53 kg of the target substance.

manufacture example 3

[0305] (Production Example 3) 2,3,5-Trimethyl-4-nitropyridine 1-oxide

[0306]

[0307] To 98% sulfuric acid (4.93 kg, 49.3 mol) was added 2,3,5-collidine 1-oxide (1.38 kg, 10.1 mol). After dripping 97% nitric acid (1.44 kg) over 50 minutes, it heated at 85 degreeC for 4 hours. The reaction solution was added to a mixture of ammonium bicarbonate (10.6 kg) and water (9.0 L), and extracted with ethyl acetate (3.0 L×3). The resulting organic layer was concentrated and vacuum-dried overnight to obtain 1.50 kg of the desired substance.

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Abstract

Salts of 2-[({4-[(2,2-dimethyl-1,3-dioxan-5-yl)methoxy]-3,5-dimethylpyridin-2-yl}methyl)sulfinyl]-1H-benzimidazole, and crystals and amorphous forms thereof.

Description

technical field [0001] The present invention relates to salts of sulfinylbenzimidazole compounds useful as gastric acid secretion inhibitors, their crystals, and amorphous forms. In addition, the present invention also relates to crystals and amorphous substances of free forms of sulfinylbenzimidazole compounds. Background technique [0002] It is generally believed that the occurrence of peptic ulcers such as gastric ulcer and duodenal ulcer is the result of autolysis caused by the destruction of the balance of attack factors such as acid and pepsin and defense factors such as mucus and blood flow. [0003] Peptic ulcer is treated internally in principle, and various drug therapies have been tried. In particular, a drug has recently been developed that can specifically block the enzyme H+, K+-ATPase present in parietal cells and in charge of the final process of gastric acid secretion, inhibit acid secretion, and prevent autolysis as a result, such as Ogilvy & Mather Praz...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D405/14
CPCC07D405/14A61P1/02A61P1/04A61P1/14A61P19/02A61P27/16A61P31/04
Inventor 川原哲也原田均寺内广毅渡边信久上田正人镰田厚菊池幸子石原比吕之小山晃一郎
Owner EISIA R&D MANAGEMENT CO LTD
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