Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT 2C receptor

Progress in the Chemistry of Tetrahydroquinolines

“…In a similar domino approach based on the combination of intramolecular S N Ar and aza-Michael steps, treatment of 1,2- or 1,3-diamines 398 with the fluorinated precursors 399 allowed the one-pot construction of the tricyclic compounds 400 (Scheme ). This work led to the identification of pyrimidine-diazabicyclo[3.3.0]­octane derivatives 401 as agonists of the serotonin 5-HT 2C receptor, which is involved in the regulation of appetite and is therefore considered as an interesting target to combat obesity …”

“…This work led to the identification of pyrimidinediazabicyclo[3.3.0]octane derivatives 401 as agonists of the serotonin 5-HT 2C receptor, which is involved in the regulation of appetite and is therefore considered as an interesting target to combat obesity. 205…”

Recent Advances in Methylation: A Guide for Selecting Methylation Reagents

“…In general, methylation occurs on an activated substrate such as C‐halides (Cl, Br), C‐OTf, C‐OSO 2 C 6 F 5 , and halogenated acrylates . In many cases, methylation is carried out on late‐stage intermediates, and more interestingly, owing to the excellent functional group tolerance, TMB‐mediated methylation chemistry is often published in journals relevant to medicinal chemistry, in which functional groups, such as secondary amine, oxetane, acetal, aldehyde, ketone, imidazole, aniline, thiol ether, indole, ester, and amide are often designed into pharmaceutical molecules or their corresponding intermediates.…”