On January 15, 2020, Larsen, Matthew A.; Hennessy, Elisabeth T.; Deem, Madeleine C.; Lam, Yu-hong; Sauri, Josep; Sather, Aaron C. published an article.Electric Literature of 517-23-7 The title of the article was A Modular and Diastereoselective 5 + 1 Cyclization Approach to N-(Hetero)Aryl Piperidines. And the article contained the following:
A new general de novo synthesis of pharmaceutically important N-(hetero)aryl piperidines is reported. This protocol uses a robustly diastereoselective reductive amination/aza-Michael reaction sequence to achieve rapid construction of complex polysubstituted ring systems starting from widely available heterocyclic amine nucleophiles and carbonyl electrophiles. Notably, the diastereoselectivity of this process is enhanced by the presence of water, and DFT calculations support a stereochem. model involving a facially selective protonation of a water-coordinated enol intermediate. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Electric Literature of 517-23-7
The Article related to heteroarylpiperidine diastereoselective preparation, aminoheteroarene ketoacrylate diastereoselective reductive amination aza michael reaction, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Electric Literature of 517-23-7
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