Tomeglovir, BAY-38-4766
托美洛韦Chemical Name: N-[4-[5-(Dimethylamino)-1-naphthylsulfonamido]phenyl]-3-hydroxy-2,2-dimethylpropionamide
CAS No. 233254-24-5
项目整合开发状态: Phase II
项目研究机构: Bayer (Originator)
合成路线:The reaction of 5-(dimethylamino)naphthalene-1-sulfonyl chloride (I) with 4-nitroaniline (II) in pyridine gives the corresponding sulfonamide (III),which is reduced at the nitro group with hydrogen over Pd/C in ethanol,yielding the expected amine (IV).Finally,this compound is condensed with 3-hydroxy-2,2-dimethylpropionic acid (V) by means of propylphosphonic anhydride (PRPA) and triethylamine in dichloromethane/ethyl acetate.
📌 参考资料/链接：
参考文献标题:Novel naphthyl-substd.and anilide-substd.sulfonamides
文献作者:Trappe,J.; Weber,O.; Eckenberg,P.; Hallenberger,S.; Bender,W.; Goldmann,S.; H鋜ter,M.; Reefschl鋑er,J.(Bayer AG)
参考来源:WO 9937609
📄 详细内容
合成路线:The reaction of 5-(dimethylamino)naphthalene-1-sulfonyl chloride (I) with 4-nitroaniline (II) in pyridine gives the corresponding sulfonamide (III),which is reduced at the nitro group with hydrogen over Pd/C in ethanol,yielding the expected amine (IV).Finally,this compound is condensed with 3-hydroxy-2,2-dimethylpropionic acid (V) by means of propylphosphonic anhydride (PRPA) and triethylamine in dichloromethane/ethyl acetate.
参考文献标题:A novel nonnucleosidic inhibitor of human cytomegalovirus replication
文献作者:Hallenberger,S.; Weber,O.; Bender,W.; Eckenberg,P.; Reefschlaeger,J.; Goldmann,S.; Trappe,J.; Haerter,M.
参考来源:Intersci Conf Antimicrob Agents Chemother 1999,Abst F940
合成路线:The reaction of 5-(dimethylamino)naphthalene-1-sulfonyl chloride (I) with 4-nitroaniline (II) in pyridine gives the corresponding sulfonamide (III),which is reduced at the nitro group with hydrogen over Pd/C in ethanol,yielding the expected amine (IV).Finally,this compound is condensed with 3-hydroxy-2,2-dimethylpropionic acid (V) by means of propylphosphonic anhydride (PRPA) and triethylamine in dichloromethane/ethyl acetate.
参考文献标题:Bay-38-4766
文献作者:Leeson,P.A.; Sorbera,L.A.; Castar,J.
参考来源:Drugs Fut 1999,24(12),1297
产品链接: CAS No. 233254-24-5››