Singh Gurpreet, Aubé Jeffrey
The University of Kansas Chemical Methodologies and Library Development Center, 2034 Becker Drive, Del Shankel Structural Biology Center, Lawrence, Kansas 66047, United States.
Org Biomol Chem. 2016 May 14;14(18):4299-303. doi: 10.1039/c6ob00598e.
A useful design element in small molecule libraries is spatial diversity, in which binding moieties are systematically directed toward different regions of three-dimensional space. One way of achieving this is through the use of conformationally diverse scaffolds onto which various binding moieties can be placed. Such scaffolds can represent synthetic challenges of their own. In this paper, we describe a new route to chiral, cyclic 1,3-diol building blocks that features silylated dithianes as relay linchpins. These diols are subsequently used for the construction of a 24-compound pilot library bearing two amino acid residues.
小分子文库中一个有用的设计元素是空间多样性，其中结合部分被系统地导向三维空间的不同区域。实现这一点的一种方法是使用构象多样的支架，在其上可以放置各种结合部分。这样的支架本身可能代表合成挑战。在本文中，我们描述了一种合成手性环状1,3 -二醇结构单元的新方法，该方法以硅烷基化二噻烷作为中继关键结构。这些二醇随后被用于构建一个包含两个氨基酸残基的24化合物先导文库。
