399559-66-1Relevant articles and documents
Copper-Catalyzed Carbonylative Synthesis of β-Homoprolines from N-Fluoro-sulfonamides
Wu, Xiao-Feng,Yin, Zhiping,Zhang, Youcan
, p. 1889 - 1893 (2020/03/24)
A new methodology for the carbonylative transformation of N-fluoro-sulfonamides into N-sulfonyl-β-homoproline esters has been described. In the presence of a catalytic amount of Cu(OTf)2, a range of β-homoproline derivatives were prepared in moderate to good yield. The reaction proceeds via the intramolecular cyclization and intermolecular carbonylation of a free carbon radical. Notably, this procedure offers the possibility to build potential functionalized bioactive molecules.
Pd-Catalyzed Intramolecular Aminoalkylation of Unactivated Alkenes: Access to Diverse N-Heterocycles
Ye, Liu,Lo, Kai-Yip,Gu, Qiangshuai,Yang, Dan
, p. 308 - 311 (2017/04/21)
A highly efficient palladium-catalyzed intramolecular aminoalkylation of unactivated alkenes in the absence of an external ligand and oxidant is described. New C-N and C(sp3)-C(sp3) bonds are formed simultaneously. This general transformation allows for construction of diverse N-heterocycles. Mechanistic studies show that the process may involve a four-membered Pd(alkyl)amido intermediate.
Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection
Kim, Dooseop,Wang, Liping,Caldwell, Charles G.,Chen, Ping,Finke, Paul E.,Oates, Bryan,MacCoss, Malcolm,Mills, Sander G.,Malkowitz, Lorraine,Gould, Sandra L.,DeMartino, Julie A.,Springer, Martin S.,Hazuda, Daria,Miller, Michael,Kessler, Joseph,Danzeisen, Renee,Carver, Gwen,Carella, Anthony,Holmes, Karen,Lineberger, Janet,Schleif, William A.,Emini, Emilio A.
, p. 3103 - 3106 (2007/10/03)
Replacement of the large hydantoin-indole moiety from our previous work with a variety of smaller heterocyclic analogues gave rise to potent CCR5 antagonists having binding affinity comparable to the hydantoin analogues. The synthesis, SAR, and biological profiles of this class of antagonists are described.