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【结 构 式】 
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【分子编号】41587 【品名】 【CA登记号】 |
【 分 子 式 】C23H18ClN5O4S 【 分 子 量 】495.94592 【元素组成】C 55.7% H 3.66% Cl 7.15% N 14.12% O 12.9% S 6.47% |
合成路线1
该中间体在本合成路线中的序号：(III)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 . |
合成路线2
该中间体在本合成路线中的序号：(III)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 . |