树枝状聚合物负载的组合化学
Dendrimer-supported combinatorial chemistry.
作者信息
Kim R M, Manna M, Hutchins S M, Griffin P R, Yates N A, Bernick A M, Chapman K T
机构信息
Department of Molecular Design and Diversity, Merck Research Laboratories, Rahway, NJ 07065, USA.
出版信息
Proc Natl Acad Sci U S A. 1996 Sep 17;93(19):10012-7. doi: 10.1073/pnas.93.19.10012.
A new methodology for the construction of combinatorial libraries is described. The approach, termed dendrimer-supported combinatorial chemistry (DCC), centers on the use of dendrimers as soluble supports. Salient features of DCC include solution phase chemistry, homogeneous purification, routine characterization of intermediates, and high support loadings. To demonstrate the feasibility of DCC, single compounds and a small combinatorial library were prepared via the Fischer indole synthesis. Excellent product yields and purities were obtained, and dendrimer-protected intermediates could be routinely analyzed by 1H and 13C NMR and by mass spectrometry. The results indicate that DCC is a general and efficient strategy for the generation of combinatorial libraries.
本文描述了一种构建组合文库的新方法。该方法称为树枝状聚合物支持的组合化学（DCC），其核心是使用树枝状聚合物作为可溶性载体。DCC的显著特点包括溶液相化学、均相纯化、中间体的常规表征以及高载体负载量。为了证明DCC的可行性，通过费歇尔吲哚合成制备了单一化合物和一个小型组合文库。获得了优异的产物产率和纯度，并且树枝状聚合物保护的中间体可以通过1H和13C NMR以及质谱进行常规分析。结果表明，DCC是生成组合文库的一种通用且有效的策略。
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