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解锁自然界的碳氢键。

Unlocking nature's C-H bonds.

作者信息

Farmer Marcus E, Laforteza Brian N, Yu Jin-Quan

机构信息

Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, United States.

Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, United States.

出版信息

Bioorg Med Chem. 2014 Aug 15;22(16):4445-52. doi: 10.1016/j.bmc.2014.05.031. Epub 2014 May 24.

DOI:10.1016/j.bmc.2014.05.031
PMID:24909676
Abstract

In an idealistic setting, it can be imagined that if every CH bond on an organic molecule could be selectively functionalized, the fields of chemical synthesis and drug discovery would be forever revolutionized. With the purpose of investigating the practicality of this idealistic scenario, our group has endeavored to unlock the potential of nature's CH bonds by developing palladium-catalyzed, site selective CH insertions that can be incorporated into both known and new catalytic cycles. To this end, we have developed a number of catalytic transformations that not only provide rapid diversification of simple starting materials and natural products through CH functionalization, but streamline the synthesis of a variety of natural products with biological activity and expand upon methods to access highly valuable enantiopure materials.

摘要

在理想情况下,可以想象,如果有机分子上的每个碳氢键都能被选择性官能化,那么化学合成和药物发现领域将永远发生变革。为了研究这种理想情况的可行性,我们团队致力于通过开发钯催化的、位点选择性的碳氢键插入反应来释放天然碳氢键的潜力,这些反应可纳入已知和新的催化循环中。为此,我们已经开发了许多催化转化反应,这些反应不仅通过碳氢键官能化实现简单起始原料和天然产物的快速多样化,还简化了具有生物活性的各种天然产物的合成,并扩展了获取高价值对映体纯材料的方法。

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