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【结 构 式】 
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【药物名称】YM-598 【化学名称】(E)-N-[6-Methoxy-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]-2-phenylethenesulfonamide potassium salt 【CA登记号】192645-26-4 (undefined isomer), 192645-27-5 (undefined isomer, Na salt) 【 分 子 式 】C24H20KN5O5S 【 分 子 量 】529.6235 |
【开发单位】Yamanouchi (Originator) 【药理作用】ANALGESIC AND ANESTHETIC DRUGS, Analgesic Drugs, Oncolytic Drugs, Prostate Cancer Therapy, Endothelin ETA Receptor Antagonists |
合成路线1
The known dichloropyrimidine derivative (I) was condensed with 2-phenylethenesulfonamide (II) in the presence of NaH in DMF to furnish the N-pyrimidinylsulfonamide (III). Displacement of the remaining chlorine of (III) by means of methanolic NaOMe provided the corresponding methyl ether (IV). The title potassium salt was then prepared by treatment of sulfonamide (IV) with ethanolic KOH.
| 【1】 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 . |