Total synthesis of squafosacin F: stereodivergent approach to mono-tetrahydrofuran acetogenins

RSC Adv. 2019 Dec 5;9(69):40368-40377. doi: 10.1039/c9ra09762g. eCollection 2019 Dec 3.

Abstract

Annonaceous acetogenins have a wide range of potential biological activities. The development of simple and diversity-oriented approaches to their synthesis is therefore important. We have achieved the first total synthesis of squafosacin F and assigned its absolute configuration. The key steps were an acid-mediated tandem intramolecular double cyclization to build the hydroxy-flanked mono-tetrahydrofuran core and decoration with the desired functionalities of the target natural product via highly stereoselective reactions.