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【结 构 式】

【分子编号】38945

【品名】4-[2-[2-(2-chloro-1H-benzimidazol-1-yl)ethoxy]ethoxy]-2,3,6-trimethylphenol

【CA登记号】

【 分 子 式 】C20H23ClN2O3

【 分 子 量 】374.867

【元素组成】C 64.08% H 6.18% Cl 9.46% N 7.47% O 12.8%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(III)

2-Chlorobenzimidazole (I) was treated with NaH in DMF and the resulting sodium salt was alkylated with 4-[2-(2-chloroethoxy)ethoxy]-2,3,6-trimethylphenol (II) to give (III). Subsequent displacement of the chlorine of (III) with N-methyl homopiperazine (IV) at 130 C produced the desired 2-(homopiperazino)benzimidazole, which was finally treated with fumaric acid in EtOH to yield the corresponding bis fumarate salt.

1 Nakano, H.; Inoue, T.; Inagaki, N.; Taguchi, T.; Satoh, T.; Kawasaki, N.; Nagai, H.; Matsumoto, H.; Miyataka, H.; Synthesis and biological activities of novel antiallergic agents with 5-lipoxygenase inhibiting action. Bioorg Med Chem 2000, 8, 2, 373.
2 Nakano, H.; Inoue, T.; Inagaki, N.; Taguchi, T.; Matsumoto, H.; Satoh, T.; Miyataka, H.; Kawasaki, N.; Synthesis of benzimidazole derivatives as antiallergic agents with 5-lipoxygenase inhibiting action. Chem Pharm Bull 1999, 47, 11, 1573.
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) 26761 2-chloroimidazo[1,2-a]pyridine; 2-chlorobenzimidazole; 2-Amino-4'-chlorodiphenylether; 2-Aminodiphenylether; 2-chloro-1H-benzimidazole 4857-06-1 C7H5ClN2 详情 详情
(II) 38944 4-[2-(2-chloroethoxy)ethoxy]-2,3,6-trimethylphenol C13H19ClO3 详情 详情
(III) 38945 4-[2-[2-(2-chloro-1H-benzimidazol-1-yl)ethoxy]ethoxy]-2,3,6-trimethylphenol C20H23ClN2O3 详情 详情
(IV) 20903 1-methyl-1,4-diazepane 4318-37-0 C6H14N2 详情 详情
Extended Information