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- W2161682196 abstract "Stereoselective synthesis of all four stereoisomers of methylated analogues 8 of the kappa-receptor agonist GR-89.696 is presented. Starting with orthogonally protected piperazine derivatives (R,R)-4 and (S,S)-4, the reaction sequence involves oxidation, reductive amination and modification of the piperazine nitrogen protective groups. The configuration of the stereocentre in alpha-position to the pyrrolidine moiety is determined by X-ray structure analysis of (R,S)-8. In receptor-binding studies with the radioligand U-69.593, the stereoisomer with (S)-configuration at both stereogenic centres (S,S)-8 displayed the highest kappa-receptor affinity with a K(i)-value of 0.67 nM." @default.
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- W2161682196 date "2001-02-01" @default.
- W2161682196 modified "2023-10-16" @default.
- W2161682196 title "Synthesis and stereoselective κ-receptor binding of methylated analogues of GR-89.696" @default.
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- W2161682196 doi "https://doi.org/10.1016/s0223-5234(00)01208-3" @default.
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