On March 25, 2010, Kajino, Masahiro; Imaeda, Toshihiro; Ono, Koji; Aso, Kazuyoshi; Tarui, Naoki published a patent.Synthetic Route of 38939-88-7 The title of the patent was Preparation of 2-aminobenzimidazole derivatives as gastric acid secretion inhibitors. And the patent contained the following:
There are disclosed acid secretion inhibitors containing compounds represented by formula [I; R1’s may be the same or different and each represents a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, an optionally substituted alkoxy group, a hydroxy group or an optionally substituted amino group; R2 represents a hydrogen atom or a substituent; R3 represents a hydrogen atom or a substituent; ring A represents an optionally substituted carbon ring or an optionally substituted heterocyclic ring; and n represents an integer of 1-4], salts thereof, or prodrugs of the compounds or salts. These compounds inhibit proton,potassium-ATPase (H+/K+-ATPase) and are useful as gastric acid secretion inhibitors. There is also provided the preventive or therapeutic method for peptic ulcer, Zollinger-Ellison syndrome, gastritis, gastroesophageal reflux disease (GERD), symptomatic gastroesophageal reflux disease (symptomatic GERD), Barrett esophagus, functional dyspepsia, gastric cancer (stomach cancer), gastric MALT lymphoma, ulcer caused by nonsteroidal antiinflammatory agents, ulcer or hyper-gastric acidity (excessive acid secretion) caused by postsurgical stress, acute stress ulcer, hemorrhagic gastritis, stress, or upper digestive tract hemorrhage by administering the compound in mammals. Thus, a solution of 666 mg benzene-1,2-diamine in 30 mL THF was treated with 1.08 g 2-isothiocyanato-1,3,5-trimethyl benzene, refluxed for 4 h, treated with 2.24 g 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride, and refluxed for 50 min to give, after workup and recrystallization from EtOAc/hexane, 253 mg N-(2,4,6-trimethylphenyl)-1H-benzimidazol-2-amine (II). II N-(4-fluoro-2,6-dimethylphenyl)-5-methoxy-4-methyl-1H-benzimidazol-2-amine (III) showed IC50 of 970 and 14 nM, resp., against H+/K+-ATPase. A tablet formulation containing I was described. The experimental process involved the reaction of 2-Chloro-4-methyl-1-nitrobenzene(cas: 38939-88-7).Synthetic Route of 38939-88-7
The Article related to aminobenzimidazole preparation gastric acid secretion inhibitor, proton potassium atpase inhibitor aminobenzimidazole preparation, peptic ulcer zollinger ellison syndrome prevention treatment aminobenzimidazole preparation, gastritis gastroesophageal reflux disease gerd prevention treatment aminobenzimidazole preparation and other aspects.Synthetic Route of 38939-88-7
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