Studies on the active conformation of the NK1 antagonist CGP 49823. Part 21. Fluoro-olefin analogs of tertiary amide rotamers.

Four fluoro-olefin analogs of CGP 49823 have been synthesized. Comparison of their binding affinities for the NK1 receptor suggests an active conformation of CGP 49823, where the aromatic ring of the benzamide has a syn orientation towards the 2-benzyl substituent.