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Communication | Special issue | Vol 67, No. 1, 2006, pp.79-83
Published online, 20th May, 2005
DOI: 10.3987/COM-05-S(T)7
Estrogen Receptor Ligands. Part 15: Synthesis of Benzothiopyran-based Selective Estrogen Receptor Alpha Modulators (SERAM)

Seongkon Kim,* Frank DiNinno, Elizabeth T. Birzin, Wanda Chan, Yi Tien Yang, and Milton L. Hammond

*Division of Merck & Co., Inc., Merck Research Laboratories, P.O.Box 2000, Rahway, NJ 07065, U.S.A.

Abstract

Benzothiopyran (2) was prepared and the bioactive (+)-2 was found to exhibit a reduced affinity toward the estrogen receptors (ERα/β) when compared to the corresponding dihydrobenzoxathiin (+)-1.