Design, synthesis, and structure–activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine

Efficient and practical asymmetric synthesis of 1-tert-butyl 3-methyl (3R,4R)-4-(2-oxo-2,3-dihydro-1H-benzimidazol-1-yl)piperidine-1,3-dicarboxylate, a useful intermediate for the synthesis of nociceptin antagonists

“…15,16 Interest in ORL-1 has resulted in an increase of publications in scientific and patent literature on related antagonists. 17,18 A decade ago, we identified a series of potent and selective non-peptide ORL-1 antagonists exemplified by J-113397 possessing two stereogenic centers on the piperidine ring ( Fig. 1).…”