Enantioselective Total Synthesis of (+)-Gephyrotoxin 287C

A synthesis of (+)-gephyrotoxin 287C using, (S)-phenylglycinol-derived tricyclic lactam 7 as the starting enantiomeric scaffold is reported. From the stereochemical standpoint, the key steps are the generation of the DHQ C-5 stereocenter by hydrogenation of the C-C double bond, removal of the chiral...

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Bibliographic Details
Authors: Piccichè, Miriam, Pinto, Alexandre, Griera Farres, Rosa, Bosch Cartes, Joan, Amat Tusón, Mercedes
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:2445/127597
Online Access:https://hdl.handle.net/2445/127597
Access Level:Open access
Keyword:Síntesi asimètrica
Lactames
Catàlisi asimètrica
Asymmetric synthesis
Lactams
Enantioselective catalysis
Description
Summary:A synthesis of (+)-gephyrotoxin 287C using, (S)-phenylglycinol-derived tricyclic lactam 7 as the starting enantiomeric scaffold is reported. From the stereochemical standpoint, the key steps are the generation of the DHQ C-5 stereocenter by hydrogenation of the C-C double bond, removal of the chiral inductor to give a cis-DHQ introduction of the DHQ C-2 substituent, completion of the (Z)-enyne moiety, and generation of the C-1 stereocenter during closure of the pyrrolidine ring.