Late-Stage Diversification of Natural Products

Benke Hong; Tuoping Luo; Xiaoguang Lei

doi:10.1021/acscentsci.9b00916

Late-Stage Diversification of Natural Products

ACS Cent Sci. 2020 May 27;6(5):622-635. doi: 10.1021/acscentsci.9b00916. Epub 2020 Apr 22.

Authors

Benke Hong^{1

2

3

4

5}, Tuoping Luo^{1

3

5

6}, Xiaoguang Lei^{1

2

3

4

5}

Affiliations

¹ Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Peking University, Beijing 100871, China.
² Department of Chemical Biology, Peking University, Beijing 100871, China.
³ College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
⁴ Synthetic and Functional Biomolecules Center, Peking University, Beijing 100871, China.
⁵ Peking-Tsinghua Center for Life Sciences, Peking University, Beijing 100871, China.
⁶ Academy for Advanced Interdisciplinary Studies, Peking University, Beijing 100871, China.

Abstract

Late-stage diversification of natural products is an efficient way to generate natural product derivatives for drug discovery and chemical biology. Benefiting from the development of site-selective synthetic methodologies, late-stage diversification of natural products has achieved notable success. This outlook will outline selected examples of novel methodologies for site-selective transformations of reactive functional groups and inert C-H bonds that enable late-stage diversification of complex natural products. Accordingly, late-stage diversification provides an opportunity to rapidly access various derivatives for modifying lead compounds, identifying cellular targets, probing protein-protein interactions, and elucidating natural product biosynthetic relationships.

Publication types

Review