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ChemInform Abstract: First Asymmetric Organocatalyzed Domino Friedel-Crafts/Lactonization Reaction in the Enantioselective Synthesis of the GABAB Receptor Modulator (S)-BHFF

Authors :
M. Antonietta Loreto
Martina Miceli
Emilia Cupioli
Fabrizio Vetica
Augusto Gambacorta
Renata Marcia de Figueiredo
Tecla Gasperi
Source :
ChemInform. 47
Publication Year :
2016
Publisher :
Wiley, 2016.

Abstract

An asymmetric domino Friedel–Crafts/lactonization sequence between phenols and trifluoropyruvate has been accomplished for the first enantioselective synthesis of ( S )-BHFF, a positive allosteric modulator (PAM) of GABA B receptor. The developed protocol leads to 3-OH-benzofuranone derivatives bearing a quaternary stereogenic center, and gives a valuable access to bioactive compounds with promising pharmaceutical applications.

Details

ISSN :
09317597
Volume :
47
Database :
OpenAIRE
Journal :
ChemInform
Accession number :
edsair.doi...........60dad7ae6702992874d785a63c100d85
Full Text :
https://doi.org/10.1002/chin.201622116