Tetrahedron letters

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

DA Bradley, AG Godfrey, CR Schmid

Index: Bradley, David A.; Godfrey, Alexander G.; Schmid, Christopher R. Tetrahedron Letters, 1999 , vol. 40, # 28 p. 5155 - 5159

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Citation Number: 36

Abstract

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.