An Assembly Concept for the Consecutive Introduction of Unsymmetrical Disulfide Bonds: Synthesis of a Releasable Multidrug Conjugate of Folic Acid

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• 作者：Iontcho R. Vlahov ; Hari Krishna R. Santhapuram ; Yu Wang ; Paul J. Kleindl ; Fei You ; Stephen J. Howard ; Elaine Westrick ; Joseph A. Reddy ; Christopher P. Leamon
• 刊名：Journal of Organic Chemistry
• 出版年：2007
• 出版时间：August 3, 2007
• 年：2007
• 卷：72
• 期：16
• 页码：5968 - 5972
• 全文大小：206K
• 年卷期：v.72,no.16(August 3, 2007)
• ISSN：1520-6904

文摘

We describe the development of methodology which allows for the introduction of a second disulfidebond into a molecular framework with a pre-existing disulfide linker system. Compounds which containan S-9-fluorenylmethyl-protected thiol and an additional disulfide linkage are deprotected in situ andtrapped with an activated thiophile. This methodology allowed for the synthesis of the first moleculepossessing two different biologically active agents covalently attached to a folate receptor targeting ligandunit via two disulfide-based release systems.