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【结 构 式】

【药物名称】BAS-118

【化学名称】N-Methyl-3-[2-(2-naphthyl)acetamido]benzamide

【CA登记号】

【 分 子 式 】C20H18N2O2

【 分 子 量 】318.37866

【开发单位】Mitsubishi Chemical (Originator)

【药理作用】Anti-Helicobacter Pylori Agents, Antiulcer Drugs, GASTROINTESTINAL DRUGS

合成路线1

2-Naphthylacetic acid (I) was converted to the corresponding acid chloride (II) upon treatment with oxalyl chloride in the presence of a catalytic amount of DMF. Subsequent coupling of acid chloride (II) with N-methyl-3-aminobenzamide (III) in pyridine furnished the target diamide.

1 Kawamura, M.; Ando, R.; Chiba, N.; 3-(Arylacetylamino)-N-methylbenzamides: A novel class of selective anti-Helicobacter pylori agents. J Med Chem 2001, 44, 25, 4468.
2 Ando, R.; et al.; 3-(Arylacetylamino)-N-methylbenzamides: New class of selective anti-Helicobacter pylori agents. 222nd ACS Natl Meet (Aug 26 2001, Chicago) 2001, Abst MEDI 248.
3 Ando, R.; Watanabe, K.; Chiba, N.; Kawamura, M. (Mitsubishi Chemical Corp.); Amide derivs.. EP 0887341; JP 1999071336 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 50657 2-Naphthylacetic acid; beta-Naphthylacetic acid 581-96-4 C12H10O2 详情 详情
(II) 13970 2-(2-Naphthyl)acetyl chloride C12H9ClO 详情 详情
(III) 51496 3-Aminobenzoylmethylamide 25900-61-2 C8H10N2O 详情 详情
Extended Information