ABT-751, E-7010
N-[2-[(4-羟基苯基)氨基]-3-吡啶基]-4-甲氧基苯磺酰胺 N-[2-[(4-羟基苯基)氨基]-3-吡啶基]-4-甲氧基苯磺酰胺单盐酸盐 Chemical Name: N-[2-(4-Hydroxyphenylamino)-3-pyridyl]-4-methoxybenzenesulfonamide
CAS No. 141430-65-1, 141450-48-8 (monoHCl)
项目整合开发状态: Phase II
项目研究机构: Eisai (Originator), Abbott (Licensee)
合成路线:The condensation of 4-aminophenol (I) with 2-chloro-3-nitropyridine (II) in DMF at 100 C gives 4-(3-nitropyridin-2-ylamino)phenol (III),which is reduced with H2 over Pd/C in THF-methanol to afford 4-(3-aminopyridin-2-ylamino)phenol (IV).Finally,this compound is condensed with 4-methoxybenzenesulfonylchloride (V) by means of pyridine in THF.
📌 参考资料/链接：
参考文献标题:Sulfonamide derivs
文献作者:Yoshino,H.; Ueda,N.; Sugumi,H.; Niijima,J.; Kotake,Y.; Okada,T.; Koyanagi,N.; Watanabe,T.; Asada,M.; Yoshimatsu,K.; Iijima,A.; Nagasu,T.; Tsukahara,K.; Kitoh,K.(Eisai Co.,Ltd.)
参考来源:EP 0472053; JP 1993039256; US 5250549; US 5292758; US 5332751; US 5434172
📄 详细内容
合成路线:The condensation of 4-aminophenol (I) with 2-chloro-3-nitropyridine (II) in DMF at 100 C gives 4-(3-nitropyridin-2-ylamino)phenol (III),which is reduced with H2 over Pd/C in THF-methanol to afford 4-(3-aminopyridin-2-ylamino)phenol (IV).Finally,this compound is condensed with 4-methoxybenzenesulfonylchloride (V) by means of pyridine in THF.
参考文献标题:Novel sulfonamides as potential,systemically active antitumor agents
文献作者:Yoshino,H.; Ueda,N.; Niijima,J.; Sugumi,H.; Kotake,Y.; Koyanagi,N.; Yoshimatsu,K.; Asada,M.; Watanabe,T.; Nagasu,T.; et al.
参考来源:J Med Chem 1992,35(13),2496-7
合成路线:The condensation of 4-aminophenol (I) with 2-chloro-3-nitropyridine (II) in DMF at 100 C gives 4-(3-nitropyridin-2-ylamino)phenol (III),which is reduced with H2 over Pd/C in THF-methanol to afford 4-(3-aminopyridin-2-ylamino)phenol (IV).Finally,this compound is condensed with 4-methoxybenzenesulfonylchloride (V) by means of pyridine in THF.
参考文献标题:E-7010
文献作者:Hoshi,A.; Castar,J.
参考来源:Drugs Fut 1993,18(11),995
产品链接: CAS No. 141430-65-1›› 产品链接: CAS No.141450-48-8››