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项目整合精选>>>Mycophenolate mofetil, RS-61443-190(HCl), ME-MPA, RS-61443, Munoloc, CellCept
Mycophenolate mofetil, RS-61443-190(HCl), ME-MPA, RS-61443, Munoloc, CellCept
吗替麦考酚酯 吗替麦考吩酯 Chemical Name: 6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-4(E)-hexenoic acid 2-(4-morpholinyl)ethyl ester; Mycophenolic acid 2-(4-morpholinyl)ethyl ester
CAS No. 128794-94-5, 115007-34-6 (deleted CAS), 140401-05-4 (deleted CAS), 116680-01-4 (HCl)
项目整合开发状态: Launched-1995
项目研究机构: Chugai (Originator), Roche (Originator), Roche Bioscience (Originator), Aspreva (Licensee), Johann Wolfgang Goethe Universit鋞 (Codevelopment)
合成路线:Commercially available mycophelonic acid (I) is converted to its chloride (II) by means of thionyl chloride in dichloromethane/DMF and then esterified with 2-(4-morpholinyl)ethanol (III) in dichloromethane.
📌 参考资料/链接:
参考文献标题:Morpholinoethylesters of mycophenolic acid and pharmaceutical compsns
文献作者:Nelson,P.H.; Gu,C.-L.L.; Allison,A.C.; Eugui,E.M.; Lee,W.A.(Syntex (USA),Inc.)
参考来源:AU 8782540; EP 0281713; JP 1988188672; US 4753935
📄 详细内容
合成路线:Commercially available mycophelonic acid (I) is converted to its chloride (II) by means of thionyl chloride in dichloromethane/DMF and then esterified with 2-(4-morpholinyl)ethanol (III) in dichloromethane.
参考文献标题:Treatment of allograft rejection with mycophenolic acid morpholinoethyl ester and derivs.Thereof
文献作者:Allison,A.C.; Eugui,E.M.; Nelson,P.H.; Gu,C.-L.L.; Lee,W.A.(Syntex (USA),Inc.)
参考来源:US 4786637
合成路线:The esterification of mycophenolic acid (I) with 2-(4-morpholinyl)ethanol (II) in refluxing dibutyl ether or refluxing dipentyl ether with azeotropic distillation of water gives the target mycophenolic ester.
参考文献标题:Method of mycophenolate mofetil preparation
文献作者:Chudlik,M.; Husek,A.(Galena AS; Ivax Corp.)
参考来源:WO 02100855
合成路线:Commercially available mycophelonic acid (I) is converted to its chloride (II) by means of thionyl chloride in dichloromethane/DMF and then esterified with 2-(4-morpholinyl)ethanol (III) in dichloromethane.
参考文献标题:Bioavailability improvement of mycophenolic acid through amino ester derivatization
文献作者:Lee,W.A.; Gu,L.; Miksztal,A.R.; Chu,N.; Leung,K.; Nelson,P.H.
参考来源:Pharm Res 1990,7(2),161-6
合成路线:Commercially available mycophelonic acid (I) is converted to its chloride (II) by means of thionyl chloride in dichloromethane/DMF and then esterified with 2-(4-morpholinyl)ethanol (III) in dichloromethane.
参考文献标题:Mycophenolate Mofetil
文献作者:Robinson,C.; Castar,J.
参考来源:Drugs Fut 1995,20(4),356
产品链接: CAS No. 128794-94-5›› 产品链接: CAS No.115007-34-6››