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【结 构 式】

【药物名称】

【化学名称】8-Chloro-10H-[1]benzofuro[3,2-b]indole-1-carboxylic acid

【CA登记号】275377-99-6

【 分 子 式 】C15H8ClNO3

【 分 子 量 】285.68891

【开发单位】Wyeth Pharmaceuticals (Originator)

【药理作用】RENAL-UROLOGIC DRUGS, Urinary Incontinence Therapy, Large Conductance BK(Ca) Channel Activators

合成路线1

The condensation between 5-chloro-3(2H)benzofuranone (I) and 2-hydrazinobenzoic acid (II) afforded the corresponding hydrazone (III). This was subjected to microwave-promoted Fischer indole cyclization in formic acid to produce the target benzofuroindole tetracyclic system.

1 Butera, J.A.; et al.; Synthesis and potassium channel opening activity of substituted 10H-benzo[4,5]furo[3,2-b]indole- and 5,10-dihydro-indeno[1,2-b]indole-1-carboxylic acids. Bioorg Med Chem Lett 2001, 11, 16, 2093.
2 Butera, J.A.; Antane, S.A.; Lennox, J.R. (Wyeth); Substd. benzofuranoindoles and indenoindoles as novel potassium channel openers. EP 1135393; US 6288099; WO 0034285 .
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) 52306 5-Chloro-3(2H)-Benzofuranone C8H5ClO2 详情 详情
(II) 47957 2-hydrazinobenzoic acid 52356-01-1 C7H8N2O2 详情 详情
(III) 52307 2-{2-[5-chloro-1-benzofuran-3(2H)-ylidene]hydrazino}benzoic acid C15H11ClN2O3 详情 详情
Extended Information