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【结 构 式】 
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【药物名称】YM-91746 【化学名称】N-[6-Methoxy-5-(2-methoxyphenoxy)-2,2'-bipyrimidin-4-yl]-1-phenyl-1(E)-butene-2-sulfonamide potassium salt 【CA登记号】192645-50-4 (undefined isomer) 【 分 子 式 】C26H24KN5O5S 【 分 子 量 】557.67768 |
【开发单位】Yamanouchi (Originator) 【药理作用】CARDIOVASCULAR DRUGS, Hypertension, Treatment of, Endothelin ETA Receptor Antagonists |
合成路线1
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 . |