Synthesis and biological evaluation of C-2 halogenated analogs of salvinorin A.
Bioorganic & Medicinal Chemistry Letters October 1, 2010 David Y W Lee, Lu Yang, Wei Xu et al.
Salvinorin A (1), the main active ingredient of Salvia divinorum, is a potent and selective κ opioid receptor (KOPR) agonist. Based on the SAR, its C-2 position is one of the key binding sites and has very little space tolerance (3-4 carbons atoms) and limited to only lipophilic groups. In our attempt to prepare PET brain imaging agent for mapping KOPR, a series of C-2 halogenated analogs have...