Natural product-like combinatorial libraries based on privileged structures. 3. The "libraries from libraries" principle for diversity enhancement of benzopyran libraries
Natural product-like combinatorial libraries based on privileged structures. 3. The "libraries from libraries" principle for diversity enhancement of benzopyran libraries
复制标题
DOI：
10.1021/ja0020355
复制
发表时间：
2000-10-18
影响因子：
15
通讯作者：
Cao, GQ
中科院分区：
文献类型：
--
作者：
Nicolaou, KC;Pfefferkorn, JA;Cao, GQ
如前两篇论文中所述，我们对构建用于化学生物学研究的天然和天然产物样库的兴趣导致了一种新的用于构建取代苯并吡喃的固相循环加载策略的发展。在这里，我们报告了一个平行的溶液相的方法，有利于提高这些非低聚苯并吡喃库的大小和多样性，使用“库从库”的原则。我们研究背后的原理使用这种串联策略构建离散的小分子库，并描述了一个聚合物辅助的溶液相（PASP）的方法，必要的影响所需的转换的发展。一旦开发出来，这种化学方法将应用于两个示范库。
As described in the preceding two papers, our interest in the construction of natural and natural product-like libraries for chemical biology studies led to the development of a new solid-phase cycloloading strategy for the construction of substituted benzopyrans. Herein, we report a parallel solution-phase method that facilitates the enhancement of both the size and diversity of these non-oligomeric benzopyran libraries using the "libraries from libraries" principle. We examine the rationale behind the use of this tandem strategy to construct discrete small molecule libraries, and describe the development of a polymer-assisted solution-phase (PASP) methodology necessary to effect the required transformations. Once developed, this chemistry is applied to two demonstration libraries.