Asymmetric synthesis of pharmaceutically relevant 1-aryl-2-heteroaryl- and 1,2-diheteroarylcyclopropane-1-carboxylates
Jack C. Sharland, Bo Wei, David J. Hardee, Timothy R. Hodges, Wei Gong, Eric A. Voight, Huw M. L. Davies
Abstract
-substituted substrates, 2-chloropyridine was required as an additive in the presence of either 4 Å molecular sieves or 1,1,1,3,3,3-hexafluoroisopropanol (HFIP). Under the optimized conditions, the cyclopropanation could be conducted in the presence of a variety of heterocycles, such as pyridines, pyrazines, quinolines, indoles, oxadiazoles, thiophenes and pyrazoles.
Topics & Concepts
CyclopropanationEnantioselective synthesisArylChemistryCatalysisCombinatorial chemistryOrganic chemistryMedicinal chemistryAlkylCyclopropane Reaction MechanismsAsymmetric Synthesis and CatalysisCatalytic Alkyne Reactions