Issue 28, 2020

Total synthesis of tubulysin U and N14-desacetoxytubulysin H

Abstract

A concise and efficient procedure for the total synthesis of tubulysin U and N14-desacetoxytubulysin H has been developed with high stereoselectivity on a gram scale. This synthesis features an elegant cascade one-pot process to install the challenging thiazole moiety and the employment of stereoselective reductions and a series of high-yield mild reactions to ensure the requisite stereochemistry, reaction scale, and yield and to avoid the vexing epimerization occurring during peptide formation.

Graphical abstract: Total synthesis of tubulysin U and N14-desacetoxytubulysin H

Associated articles

Supplementary files

Article information

Article type
Communication
Submitted
29 ሜይ 2020
Accepted
02 ጁላይ 2020
First published
03 ጁላይ 2020

Org. Biomol. Chem., 2020,18, 5349-5353

Total synthesis of tubulysin U and N14-desacetoxytubulysin H

B. Long, C. Tao, Y. Li, X. Zeng, M. Cao and Z. Wu, Org. Biomol. Chem., 2020, 18, 5349 DOI: 10.1039/D0OB01109F

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