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【结 构 式】 
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【药物名称】YM-62899 【化学名称】N-[6-(2-Fluoroethoxy)-5-(2-methoxyphenoxy)-2,2'-bipyrimidin-4-yl]-2-phenylethenesulfonamide 【CA登记号】192645-19-5 【 分 子 式 】C25H22FN5O5S 【 分 子 量 】523.54699 |
【开发单位】Yamanouchi (Originator) 【药理作用】CARDIOVASCULAR DRUGS, Heart Failure Therapy, Hypertension, Treatment of, Endothelin ETA Receptor Antagonists |
合成路线1
Nucleophilic substitution of the dichloropyrimidine derivative (I) with 2-phenylvinylsulfonamide (II) in the presence of NaH in DMF affords the sulfonamido pyrimidine (III). The remaining chloro group of (III) is subsequently displaced with the sodium alkoxide derived from 2-fluoroethanol (IV) to provide the target fluoroethyl ether.
| 【1】 Harada, H.; Kazami, J.-I:; Watanuki, S.; Tsuzuki, R.; Yanagisawa, I.; Sudoh, K.; Tsukamoto, S.-I.; Tanaka, A.; Fujimori, A.; Ethenesulfonamide derivatives, a novel class of orally active endothelin-A receptor antagonists. Chem Pharm Bull 2001, 49, 5, 606. |
| 【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 . |
Extended Information