1,3-Diaxially Substituted <i>trans</i>-Decalins: Potential Nonsteroidal Human Progesterone Receptor Inhibitors
2008-10-03T00:00:00Z (GMT) by
On the basis of molecular modeling and QSAR analysis of the known human progesterone receptor (hPR) inhibitor Mifepristone (RU-486) and other hPR ligands, a new class of potential nonsteroidal hPR inhibitors was designed. The parent racemic compound <b>1</b> was synthesized through an efficient 13-step synthetic pathway. The key constructive steps are a stereoselective epoxide ring opening and the reductive Heck cyclization to form the main framework of (±)-<b>1</b>. The current established flexible synthetic route allows for further chemical diversification.
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