Synergistic methodologies for the synthesis of 3-aroyl-2- arylbenzo[b]thiophene-based selective estrogen receptor modulators. Two concise syntheses of raloxifene

Article abstract of DOI:10.1016/S0040-4039(99)00955-7

Difunctionalized benzo[b]thiophene intermediates are prepared which allow fully independent elaboration of the 2-aryl position or the tether position of benzo[b]thiophene-based selective estrogen receptor modulators (SERMs). Two concise syntheses of the SERM raloxifene (Evista) are presented.