8-Aminocyclazocine analogues: synthesis and structure-activity relationships.
作者： Mark P Wentland , Guoyou Xu , Christopher L Cioffi , Yingchun Ye , Wenhu Duan
DOI: 10.1016/S0960-894X(99)00670-8
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摘要: Abstract Opioid binding affinities were assessed for a series of cyclazocine analogues where the prototypic 8-OH substituent was replaced by amino and substituted-amino groups. For μ κ opioid receptors, secondary amine derivatives having (2 R ,6 ,11 )-configuration had highest affinity. Most targets efficiently synthesized from triflate or its enantiomers using Pd-catalyzed amination procedures.
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