Asymmetric Synthesis Using tert-Butanesulfinamide

使用叔丁亚磺酰胺的不对称合成

• 批准号: 0139468
• 负责人: Jonathan Ellman
• 金额: $ 33万
• 依托单位: University of California-Berkeley
• 依托单位国家: 美国
• 项目类别: Continuing Grant
• 财政年份: 2002
• 资助国家: 美国
• 起止时间: 2002-02-01 至 2005-01-31
• 项目状态: 已结题
• 来源: https://www.nsf.gov/awardsearch/showAward?AWD_ID=0139468&HistoricalAwards=false
• 关键词: Asymmetric; Synthesis; Using; tert; Butanesulfinamide

The foci of this research are fourfold and all involve the development of methodology based on the use of chiral tert-butanesulfinamide. The goals include: Asymmetric synthesis and applications of highly substituted beta-amino acids; reactions of metalloenamines derived from tert-butanesulfinyl imines, in particular for the synthesis of 1,3-amino alcohols; parallel asymmetric synthesis of amines in solution and solid support for the rapid preparation of natural products and compounds with interesting biological properties; development of tert-butanesulfinamide derived ligands as a new class of ligands for asymmetric catalysis.With this award, the Organic and Macromolecular Chemistry Program is supporting the research of Dr. Jonathan A. Ellman of the Department of Chemistry at the University of California, Berkeley. Professor Ellman will focus his work on exploring the applications of tert-butanesulfinamide to asymmetric synthesis. Since more than 75% of drugs and drug candidates contain amine functionality, the work could have significant impact on the pharmaceutical industry. The research also provides an excellent training ground for students in current organic synthesis.

本研究的焦点是四重的，都涉及的方法的基础上使用手性叔丁亚磺酰胺的发展。 这些目标包括：高度取代的β-氨基酸的不对称合成和应用;衍生自叔丁烷亚磺酰基亚胺的金属烯胺的反应，特别是用于合成1，3-氨基醇;在溶液和固体载体中的胺的平行不对称合成，用于快速制备具有感兴趣的生物学性质的天然产物和化合物;开发了叔丁亚磺酰胺衍生的配体作为一类新的不对称催化配体。有了这个奖项，有机和大分子化学计划支持乔纳森·A.加州大学伯克利分校化学系的埃尔曼说。 Ellman教授将专注于探索叔丁基亚磺酰胺在不对称合成中的应用。 由于超过75%的药物和候选药物含有胺官能团，这项工作可能对制药行业产生重大影响。 本研究也为当前有机合成专业的学生提供了一个很好的训练平台。