A novel synthetic protocol for the synthesis of pulvinones, and naturally occurring Aspulvinone E, molecules of medicinal interest

Autor: Sotirios Katsamakas, John Markopoulos, Kyriakos C. Prousis, Olga Igglessi-Markopoulou
Rok vydání: 2021
Předmět:
DOI: 10.6084/m9.figshare.17000727.v1
Popis: A novel two step methodology for readily accessible natural ���pulvinone��� derivatives in excellent yields has been developed starting from activated precursors, bearing a functionalized 1,3-dioxolane-2,4-diones (OCA���s), as dually protected-activated synthons of ��-hydroxy acids. The present procedure is based on a tandem C-acylation-cyclization process under mild conditions with good yields. Additionally, pulvinones show an important medicinal profile with the tetronate heterocycle exhibiting favorable pharmacokinetic (PK) and ADME-Tox properties that can be considered unexploited so far due to synthetic limitations.
Databáze: OpenAIRE