Hayashi, Shigeo; Hirao, Akiko; Imai, Aki; Nakamura, Hiroshi; Murata, Yoshinori; Ohashi, Katsuyo; Nakata, Eriko published an article on February 11 ,2009. The article was titled 《Novel Non-Peptide Nociceptin/Orphanin FQ Receptor Agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: Design, Synthesis, and Structure-Activity Relationship of Oral Receptor Occupancy in the Brain for Orally Potent Antianxiety Drug》, and you may find the article in Journal of Medicinal Chemistry.Application In Synthesis of (R)-1-tert-Butyl 3-ethyl piperidine-1,3-dicarboxylate The information in the text is summarized as follows:
An endogenous heptadecapeptide, nociceptin/orphanin FQ (N/OFQ), and a G-protein-coupled receptor, N/OFQ peptide (NOP) receptor [or opioid-receptor-like-1 (ORL1) receptor], have been described in terms of its structure, distribution, and pharmacol. Thus, the N/OFQ and NOP receptor are located in the central nervous systems in humans, primates, and rodents, and are involved in the integration of the emotional components in the brain; e.g., N/OFQ displays anxiolytic activity in the brain. For identifying orally potent anxiolytic, drug-design studies were performed with a series of 1,2-disubstituted benzimidazole derivatives, which resulted in the identification of various chemotypes of highly potent NOP selective full agonists in vitro with high or moderate NOP receptor occupancy in the mice brain per os such as 1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole (MCOPPB), the most potent novel non-peptide NOP full agonist in vitro and an orally potent anxiolytic in the mice. The experimental part of the paper was very detailed, including the reaction process of (R)-1-tert-Butyl 3-ethyl piperidine-1,3-dicarboxylate(cas: 194726-40-4Application In Synthesis of (R)-1-tert-Butyl 3-ethyl piperidine-1,3-dicarboxylate)
(R)-1-tert-Butyl 3-ethyl piperidine-1,3-dicarboxylate(cas: 194726-40-4) is a member of piperidine. Piperidine is ubiquitous structural motif widely occurred in diverse synthetically and naturally occurring bioactive molecules. Piperidines are an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.Application In Synthesis of (R)-1-tert-Butyl 3-ethyl piperidine-1,3-dicarboxylate
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem