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paecilospirone

National Institutes of Health

Papers overview

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2013
2013
Endophytic fungi are a prolific source of metabolites with significant biological activities. As part of our systematic search… 
2012
2012
Two cycloaddition strategies are described that lead to various chroman spiroketals from assorted exocyclic enol ethers. Unlike… 
2011
2011
Review
2011
Review
2011
...................................................................................................................................... ii Acknowledgements .................................................................................................................... iv Abbreviations ........................................................................................................................... viii CHAPTER ONE: INTRODUCTION 1.1 Cancer in Modern Society ...................... ................................................................................3 1.1.1 Cancer Therapy: Targeting the Cell Cycle .. ..... ......................................................3 1.2 Paecilospirone – Isolation, Structure and Bios ynthesis ......................................... ...............5 1.3 Previous Syntheses Related to Paecilospirone ......................................................................7 A Clark-Lewis and McGarry ...................................................................................7 B Pettus and co-workers ......................... ...............................................................7 1.4 Aim of the Present Research ................. ................................................................................8 1.5 The Chemistry of Asymmetric Aldol Reactions ... ... ...........................................................9 1.5.1 Asymmetric Induction From the Aldehyde ..... . .................................................. 11 1.5.2 Asymmetric Induction From the Enolate ........................................................... 13 A Substrate-Mediated Aldol Reactions ........... ................................................... 13 B Auxiliary-Mediated Aldol Reactions ........... .................................................. 14 C Ligand-Mediated Aldol Reactions ........................................................... 17 1.5.3 Asymmetric Induction From a Chiral Lewis Aci d .................................................. 18 1.6 Retrosynthesis of Aldehyde Fragment 11 ............................................................................ 21 CHAPTER TWO: DISCUSSION 2.1 Synthesis of Spiroacetals 114 and 115 via an Acid-Catalysed Spirocyclisation Approach ...... 25 2.1.1 Overview ................................... .............................................................................. 25 2.1.2 Synthesis of Aldehyde 68 ........................................................................................ 26 2.1.3 Synthesis of Chiral Imide 48 .................................................................................. 29 2.1.4 Synthesis of Aldehyde 96 ........................................................................................ 30 A Using a Lewis Acid-Mediated Aldol Reaction .... . ...................................... 30 B Using a Magnesium Chloride-Catalysed anti-Aldol Reaction ........................ 32 C Using a Lactate-Derived anti-Aldol Reaction ............................................ 35 2.1.5 Synthesis of Bromide 99 ......................................................................................... 38