Formal total synthesis of amphidinolide E

A formal total synthesis of the cytotoxic macrolide amphidinolide E is reported. The strategic steps are three Julia-Kocienski reactions (J-K), for the formation of the C5-C6, C9-C10, and C17-C18 double bonds, a Suzuki-Molander C21-C22 bond formation reaction, and a Kita-Trost macrolactonization. Th...

Full description

Bibliographic Details
Authors: Bosch Hereu, Lluís, Mola Solà, Laura, Petit Roig, Elena, Saladrigas, Mar, Esteban Jarne, Jordi, Costa i Arnau, Anna M., Vilarrasa i Llorens, Jaume
Format: article
Status:Versión aceptada para publicación
Publication Date:2017
Country:España
Institution:Universidad de Barcelona
Repository:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/154828
Online Access:https://hdl.handle.net/2445/154828
Access Level:Open access
Keyword:Síntesi orgànica
Enllaços químics
Organic synthesis
Chemical bonds
Description
Summary:A formal total synthesis of the cytotoxic macrolide amphidinolide E is reported. The strategic steps are three Julia-Kocienski reactions (J-K), for the formation of the C5-C6, C9-C10, and C17-C18 double bonds, a Suzuki-Molander C21-C22 bond formation reaction, and a Kita-Trost macrolactonization. The 'instability' of the two dienic systems and of the stereocenter at C2 (allylic methine, alpha to the carboxy group) and the protecting groups at C17-OH and C18-OH have posed difficult challenges. Each Julia-Kocienski olefination has been systematically optimized to provide the highest possible E/Z ratios.