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新产品编号:2487413

Chemical Name: N1-[2-Hydroxytetrahydrofuran-3(S)-yl]-N2-(phenylaminocarbonothioyl)-L-leucinamide
项目整合开发状态: Preclinical
项目研究机构: Senju (Originator)
合成路线:N-Boc-L-Leucine (I) is activated as the corresponding succinimidyl ester (II) upon treatment with N-hydroxysuccinimide and EDC.Coupling of active ester (II) with (S)-alpha-amino-gamma-butyrolactone (III) affords amide (IV).After N-Boc group deprotection of (IV) under acidic conditions,the resultant amine (V) is condensed with phenyl isothiocyanate to furnish thiourea (VI).Finally,reduction of the lactone function of (VI) with DIBAL gives rise to the target cyclic hemiacetal compound.
📌 参考资料/链接:
参考文献标题:Exploration of cornea permeable calpain inhibitors as anticataract agents
文献作者:Nakamura,M.; Yamaguchi,M.; Sakai,O.; Inoue,J.
参考来源:Bioorg Med Chem 2003,11(7),1371