Author/Authors :
Paul E. Finke، نويسنده , , Laura C. Meurer، نويسنده , , Dorothy A. Levorse، نويسنده , , Sander G. Mills، نويسنده , , Malcolm MacCoss، نويسنده , , Sharon Sadowski، نويسنده , , Margaret A. Cascieri، نويسنده , , Kwei-Lan Tsao، نويسنده , , Gary G. Chicchi، نويسنده , , Joseph M. Metzger، نويسنده , , D. Euan MacIntyre، نويسنده ,
Abstract :
An initial investigation of the novel cyclopentane scaffold 6 afforded low nanomolar human NK1 antagonists having enhanced water solubility properties compared to morpholine 1. A synthesis of this cyclopentane scaffold, having three contiguous chiral centers, and the unexpected determination that the 1,2-trans-2,3-trans-ring stereochemistry, as opposed to the cis-ether/phenyl configuration of the known structures 1–5, is optimal for this class of antagonist are described.
