Improvement of σ1 receptor affinity by late-stage C-H-bond arylation of spirocyclic lactones

Article abstract of DOI:10.1016/j.bmc.2013.01.038

The direct C-H-bond arylation of the complex spirocyclic lactones 13, 14, and 18 allows the introduction of diverse aryl moieties in the last step of the synthesis. A selective α-arylation of the thiophene moiety was performed with the catalytic system Pd