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【结 构 式】

【分子编号】28291

【品名】2-[[3-(chloromethyl)phenoxy]methyl]-1-(2-ethoxyethyl)-1H-benzimidazole

【CA登记号】

【 分 子 式 】C19H21ClN2O2

【 分 子 量 】344.84072

【元素组成】C 66.18% H 6.14% Cl 10.28% N 8.12% O 9.28%

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:(IV)

Alkylation of 3-hydroxybenzyl alcohol (II) with benzimidazolylmethyl chloride (I) in the presence of K2CO3 and tetrabutylammonium bromide provided ether (III). The hydroxyl group of (III) was converted to chloride (IV) by treatment with thionyl chloride. Finally, alkylation of hydroxybenzothiazinone (V) with chloride (IV) yielded the title compound.

1 Tamura, M.; Tohma, T.; Onogi, K.; et al.; VUF-K-8707 and analogs, non-acidic leukotriene D4 receptor antagonists. 15th European Federation for Medicinal Chemistry International Symposium on Medicinal Chemistry (Sept 6 1998, Edinburgh) 1998, Abst P.226.
2 Timmerman, H.; Zhang, M.; Onogi, K.; Tamura, M.; Toma, T.; Wada, Y. (Kowa Co., Ltd.); Heteroaryl substd. phenylene derivs., their preparation and their use a leukotriene receptor antagonists. EP 0799826; JP 1997323975; US 5756518; US 5885987; US 6011033 .
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) 28288 2-(chloromethyl)-1-(2-ethoxyethyl)-1H-benzimidazole C12H15ClN2O 详情 详情
(II) 17296 3-Hydroxybenzyl alcohol; 3-(hydroxymethyl)phenol 620-24-6 C7H8O2 详情 详情
(III) 28289 (3-[[1-(2-ethoxyethyl)-1H-benzimidazol-2-yl]methoxy]phenyl)methanol C19H22N2O3 详情 详情
(IV) 28291 2-[[3-(chloromethyl)phenoxy]methyl]-1-(2-ethoxyethyl)-1H-benzimidazole C19H21ClN2O2 详情 详情
(V) 28290 7-hydroxy-2H-1,4-benzothiazin-3(4H)-one C8H7NO2S 详情 详情
Extended Information