title: Solid-phase synthesis of N-formylhydroxylamines (reverse/retro-hydroxamates).
abstract: N-Formylhydroxylamines, also known as reverse- or retro-hydroxamates, have become of significant interest in the recent past as inhibitors of metalloenzymes. Although solution-phase synthetic routes to such compounds have been reported, these are often lengthy and involve purification at each stage. Herein, novel three-step solid-phase synthetic approaches are described that enable libraries of such compounds to be produced in a convergent and efficient manner using commercially available starting materials. [reaction: see text]
authors.affiliation: Argenta Discovery Ltd., 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex, CM19 5TR, UK.
authors.forename: Steve
authors.initials: S
authors.lastname: Price
authors.forename: Susan E
authors.initials: SE
authors.lastname: Osbourn
mesh_terms: D020650:Combinatorial Chemistry Techniques; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008667:Metalloproteins / Q000037:antagonists & inhibitors*; D015394:Molecular Structure
chemical_list: D004791:Enzyme Inhibitors; D006877:Hydroxamic Acids; D008667:Metalloproteins