215673-31-7Relevant articles and documents
Synthesis and biological activity of trans-2,3-dihydroraloxifene
Schmid, Christopher R.,Glasebrook, Andrew L.,Misner, Jerry W.,Stephenson, Gregory A.
, p. 1137 - 1140 (1999)
The synthesis and biological evaluation of trans-2,3-dihydroraloxifene, 2, is described. The synthesis proceeds in 8 steps in 20% overall yield. Relative trans 2,3-stereochemistry is definitively established in ester 6, which is converted to the title compound via derivatization, Grignard addition, and deprotection. Evaluation in vitro shows the compound to be a potent selective estrogen receptor modulator (SERM).