Synthesis of oxaspiropiperidines as a strategy for lowering logD

T Cernak, K Dykstra, D Levorse, A Verras, J Balkovec…

Index: Cernak, Timothy; Dykstra, Kevin; Levorse, Dorothy; Verras, Andreas; Balkovec, James; Nargund, Ravi; DeVita, Robert Tetrahedron Letters, 2011 , vol. 52, # 48 p. 6457 - 6459

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Abstract

Spiropiperidines have emerged as valuable fragments for drug discovery and have demonstrated favorable biological properties in small molecule programs across multiple therapeutic areas. 1 Spiropiperidine frameworks are often described as privileged structures 2 because they have been successfully employed as ligands for a variety of targets including muscarinic, 3 δ-opioid, 4 melanocortin, 5 and CCR4 receptors, 6 as well as the proteins HDAC, 7 ACC, ...