Fesoterodine, SPM-907
弗斯特罗定Chemical Name: 2-Methylpropionic acid 2-[3-(N,N-diisopropylamino)-1(R)-phenylpropyl]-4-(hydroxymethyl)phenyl ester; Isobutyric acid 2-[3-(diisopropylamino)-1(R)-phenylpropyl]-4-(hydroxymethyl)phenyl ester
CAS No. 286930-02-7, 345663-07-2 (hydrochloride), 286930-04-9 (hydrochloride hydrate), 286930-03-8 (maleate)
项目整合开发状态: Phase III
项目研究机构: Schwarz (Originator)
合成路线:The known aminoacid (I) is esterified to (II) employing methanolic H2SO4.Ester group reduction in (II) with LiAlH4 yields alcohol (III).The O-benzyl group of (III) is then removed by catalytic hydrogenation in the presence of Raney nickel,providing phenol (V).Alternatively,compound (III) is converted into diol (V) by O-benzyl group hydrogenolysis,followed by LiAlH4 reduction of the resultant ester (IV).Finally,selective monoesterification of diol (V) with isobutyryl chloride (VI) and triethylamine gives rise to the title compound.
📌 参考资料/链接：
参考文献标题:Stable salts of novel derivs.of 3,3-diphenylpropylamines
文献作者:Meese,C.(Schwarz Pharma AG)
参考来源:DE 19955190; JP 2003514018; WO 0135957
📄 详细内容
合成路线:The known aminoacid (I) is esterified to (II) employing methanolic H2SO4.Ester group reduction in (II) with LiAlH4 yields alcohol (III).The O-benzyl group of (III) is then removed by catalytic hydrogenation in the presence of Raney nickel,providing phenol (V).Alternatively,compound (III) is converted into diol (V) by O-benzyl group hydrogenolysis,followed by LiAlH4 reduction of the resultant ester (IV).Finally,selective monoesterification of diol (V) with isobutyryl chloride (VI) and triethylamine gives rise to the title compound.
参考文献标题:Fesoterodine
文献作者:Sorbera,L.A.; Castar,J.; Leeson,P.A.
参考来源:Drugs Fut 2003,28(7),647
产品链接: CAS No. 286930-02-7››