Applications of Sulfonamides and Sulfinamides to Small Molecule Library Synthesis

所提出的研究包括开发基于固体载体的小分子文库的合成方法。在NSF支持的早期工作中，开发了一种N-酰基磺酰胺连接物，它允许在最后一步中化学选择性地激活文库成员的亲核释放。这一发展现在将扩展到含有氨基酸和多肽的文库。立体化学定义的化合物将通过连接光学活性构建块和通过在固体载体上合成不对称中心来生成。有了这一续期奖项，有机和高分子化学项目将继续支持加州大学伯克利分校化学系乔纳森·A·埃尔曼博士的研究。这项研究的重点是开发改进的组合方法来合成小分子文库，这些方法可用于药物发现、分子识别、材料开发和催化等领域。研究生将接受有机合成和组合化学方面的宝贵培训，这将为他们在几个快速增长的行业中的职业生涯做好准备。

The research proposed involves the development of methods for the synthesis of small molecule libraries based on solid supports. In earlier NSF supported work, an N-acylsulfonamide linker was developed which allowed chemoselectively activated nucleophilic release of library members in a final step. This development will now be extended to libraries incorporating amino acids and peptides. Stereochemicaly defined compounds will be generated both by linking optically active building blocks and by synthesizing asymmetric centers on the solid supports. With this renewal award, the Organic and Macromolecular Chemistry Program is continuing support for the research of Dr. Jonathan A. Ellman in the Department of Chemistry at the University of California at Berkeley. The research focuses on developing improved combinatorial methods for the synthesis of libraries of small molecules which can be useful in the fields of drug discovery, molecular recognition, materials development, and catalysis. Graduate students will receive valuable training in organic synthesis and combinatorial chemistry, which will prepare them for careers in several rapidly growing industries.