title: An atom-efficient and convergent approach to the preparation of NS5A inhibitors by C-H activation.
abstract: A novel approach of the convergent functionalisation of aryl dibromides to form NS5A type inhibitors using C-H activation is reported. The focus of investigation was to reduce the formation of homodimeric side product, as well as to investigate the scope of different aryl dibromides that were tolerated under the reaction conditions. The C-H activation methodology was found to give a viable synthetic route to NS5A inhibitors, with late stage functionalisation of the core portion of the molecule, albeit with some chemical functionalities not tolerated.
authors.affiliation: Sussex Drug Discovery Centre, University of Sussex, Brighton, England BN1 9QJ, UK. T.Moore@sussex.ac.uk.
authors.forename: Thomas O
authors.initials: TO
authors.lastname: Moore
authors.affiliation: Sussex Drug Discovery Centre, University of Sussex, Brighton, England BN1 9QJ, UK. T.Moore@sussex.ac.uk.
authors.forename: Michael
authors.initials: M
authors.lastname: Paradowski
authors.affiliation: Sussex Drug Discovery Centre, University of Sussex, Brighton, England BN1 9QJ, UK. T.Moore@sussex.ac.uk.
authors.forename: Simon E
authors.initials: SE
authors.lastname: Ward
mesh_terms: D004305:Dose-Response Relationship, Drug; D006842:Hydrocarbons, Brominated / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*; D012324:RNA-Dependent RNA Polymerase
chemical_list: D006842:Hydrocarbons, Brominated; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase