Photochemical Synthesis of N-Arylbenzophenanthridine Selective Estrogen Receptor Modulators (SERMs)
Journal of Medicinal Chemistry2001Vol. 44(17), pp. 2857–2860
Citations Over TimeTop 19% of 2001 papers
Timothy A. Grese, Mary D. Adrian, Diane L. Phillips, Pamela K. Shetler, Lorri L. Short, Andrew L. Glasebrook, Henry U. Bryant
Abstract
Selective estrogen receptor modulators are an emerging class of pharmaceutically important molecules. Many compounds in this class contain an aminoethoxyaryl moiety attached to a polycyclic framework at an asymmetric carbon atom. To assess whether this carbon atom can be replaced by nitrogen, we have employed a Ninomiya enamide photocyclization for the rapid synthesis of a novel N-arylbenzophenanthridine framework, 4. Further elaboration of 4 into a new structural class of achiral, nonsteroidal estrogen receptor modulators is described.
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