Deconstructive and Divergent Synthesis of Bioactive Natural Products

Author:

Hou Si-Hua1ORCID,Zhou Feng-Fan1,Sun Yi-Hang1,Li Quan-Zhe1

Affiliation:

1. Shanghai Key Laboratory of Chiral Drugs and Engineering, College of Pharmaceutical Sciences, Shanghai Jiao Tong University, Shanghai 200240, China

Abstract

Natural products play a key role in innovative drug discovery. To explore the potential application of natural products and their analogues in pharmacology, total synthesis is a key tool that provides natural product candidates and synthetic analogues for drug development and potential clinical trials. Deconstructive synthesis, namely building new, challenging structures through bond cleavage of easily accessible moieties, has emerged as a useful design principle in synthesizing bioactive natural products. Divergent synthesis, namely synthesizing many natural products from a common intermediate, can improve the efficiency of chemical synthesis and generate libraries of molecules with unprecedented structural diversity. In this review, we will firstly introduce five recent and excellent examples of deconstructive and divergent syntheses of natural products (2021–2023). Then, we will summarize our previous work on the deconstructive and divergent synthesis of natural products to demonstrate the high efficiency and simplicity of these two strategies in the field of total synthesis.

Funder

Shanghai Jiao Tong University

China Postdoctoral Science Foundation

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

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