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【结 构 式】 
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【分子编号】59918 【品名】(E)-1-phenyl-1-butene-2-sulfonamide 【CA登记号】 |
【 分 子 式 】C10H13NO2S 【 分 子 量 】211.28476 【元素组成】C 56.85% H 6.2% N 6.63% O 15.14% S 15.18% |
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)The sulfonation of 1-phenyl-1-butene (I) with sulfuryl chloride in hot DMF provided sulfonyl chloride (II), which was then treated with ammonium hydroxyde to give sulfonamide (III). Coupling of the known dichloro bipyrimidinyl derivative (IV) with the sodium salt of sulfonamide (III) yielded the N-pyrimidinyl sulfonamide (V). The remaining chloride was then displaced with sodium methoxide in DMF, and the resultant sulfonamide was finally converted to the potassium salt with ethanolic KOH.
| 【1】 Harada, H.; Kazami, J.-I.; Watanuki, S.; Tsuzuki, R.; Sudoh, K.; Fujimori, A.; Tokunaga, T.; Tanaka, A.; Tsukamoto, S.-I.; Yanagisawa, I.; Synthesis and structure-activity relationships in a series of ethenesulfonamide derivatives, a novel class of endothelin receptor antagonists. Chem Pharm Bull 2001, 49, 12, 1593. |
| 【2】 Harada, H.; Kazami, J.; Watanuki, S.; Tsuzuki, R.; Sudou, K.; Tanaka, A. (Yamanouchi Pharmaceutical Co., Ltd.); Arylethenesulfonamide derivs. and drug compsn. containing the same. EP 0882719; US 6083955; WO 9722595 . |
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