126275-19-2Relevant articles and documents
(E)-Alkenes as replacements of amide bonds: Development of novel and potent acyclic CGRP receptor antagonists
Kim, June J.,Wood, Michael R.,Stachel, Shawn J.,De Leon, Pablo,Nomland, Ashley,Stump, Craig A.,McWherter, Melody A.,Schirripa, Kathy M.,Moore, Eric L.,Salvatore, Christopher A.,Selnick, Harold G.
, p. 258 - 261 (2014)
A new class of CGRP receptor antagonists was identified by replacing the central amide of a previously identified anilide lead structure with ethylene, ethane, or ethyne linkers. (E)-Alkenes as well as alkynes were found to preserve the proper bioactive conformation of the amides, necessary for efficient receptor binding. Further exploration resulted in several potent compounds against CGRP-R with low susceptibility to P-gp mediated efflux.
Kolbe Anodic Decarboxylation as a Green Way to Access 2-Pyrrolidinones
Goodall, Iain,Lam, Kevin,Markó, István,Quertenmont, Mathilde,Riant, Olivier
, (2020)
Nootropic compounds are a group of pharmacologically active pyrrolidones. These molecules, which enhance cognition properties and possess a large prescription field, are particularly interesting synthetic targets for the pharmaceutical industry. In this Article, we disclose an effective and environmentally friendly pyrrolidinone synthesis using electrosynthesis. The newly developed methodology includes a Kolbe decarboxylation, followed by an intramolecular radical cyclization and a radical-radical cross-coupling.
N,2,3,4-Tetrasubstituted Pyrrolidines through Tandem Lithium Amide Conjugate Addition/Radical Cyclization/Oxygenation Reactions
Kafka, Franti?ek,Pohl, Radek,Císa?ová, Ivana,Mackman, Richard,Bahador, Gina,Jahn, Ullrich
supporting information, p. 3862 - 3871 (2016/08/16)
Enantioselective syntheses of densely functionalized pyrrolidines deriving their chirality from (R)-1-(phenyl)ethylamine are reported. Allylic amines and β-substituted-α,β-unsaturated esters are used as the building blocks in this one-pot reaction. Single
