Total synthesis of bysspectin A. Issue 23 (7th June 2019)

• Record Type: Journal Article
• Authors: Yang, Feilong; Liu, Xiaoyu; Shi, Xiang; Wang, Yong; Hu, Guoru; Lin, Sheng; Jiao, Xiaozhen; Xie, Ping
• Is Part Of: Tetrahedron. Volume 75:Issue 23(2019)
• Page Start: 3101
• Page End: 3107
• Publication Date: 2019-06-07
• Subjects: Bysspectin A -- Total synthesis -- hCE2 inhibitor -- Domino sonogashira-cyclization; Chemistry, Organic -- Periodicals; 547.005
• DOI: 10.1016/j.tet.2019.04.047
• Languages: English
• ISSNs: 0040-4020

Abstract

Abstract: Bysspectin A (1), an unusual polyketide-derived octaketide dimer, has highly selective inhibitory activities against human carboxylesterase 2 (hCE2) with an IC50 value of 2.01 μM. Herein, we report the first synthesis of this natural product. The synthesis relies upon a key Cu-catalysed domino Sonogashira-cyclization process. Graphical abstract: Image 1