142374-19-4Relevant articles and documents
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: Modifications of the arylpropylpiperidine side chains
Lynch, Christopher L.,Willoughby, Christopher A.,Hale, Jeffrey J.,Holson, Edward J.,Budhu, Richard J.,Gentry, Amy L.,Rosauer, Keith G.,Caldwell, Charles G.,Chen, Ping,Mills, Sander G.,MacCoss, Malcolm,Berk, Scott,Chen, Liya,Chapman, Kevin T.,Malkowitz, Lorraine,Springer, Martin S.,Gould, Sandra L.,DeMartino, Julie A.,Siciliano, Salvatore J.,Cascieri, Margaret A.,Carella, Anthony,Carver, Gwen,Holmes, Karen,Schleif, William A.,Danzeisen, Renee,Hazuda, Daria,Kessler, Joseph,Lineberger, Janet,Miller, Michael,Emini, Emilio A.
, p. 119 - 123 (2003)
The 4-(3-phenylprop-1-yl)piperidine moiety of the 1,3,4-trisubstituted pyrrolidine CCR5 antagonist 1 was modified with electron deficient aromatics as well as replacement of the benzylic methylene with sulfones, gem-difluoromethylenes and alcohols in an effort to balance the antiviral potency with reasonable pharmacokinetics.
Exploiting Synergistic Catalysis for an Ambient Temperature Photocycloaddition to Pyrazoles
Lakeland, Christopher P.,Watson, David W.,Harrity, Joseph P. A.
supporting information, p. 155 - 159 (2019/12/11)
Sydnone-based cycloaddition reactions are a versatile platform for pyrazole synthesis, however they operate under harsh conditions (high temperature and long reaction times). Herein we report a strategy that addresses this limitation utilizing the synergistic combination of organocatalysis and visible-light photocatalysis. This new approach proceeds under ambient conditions and with excellent levels of regiocontrol. Mechanistic studies suggest that photoactivation of sydnones, rather than enamines, is key to the successful implementation of this process.
OXOPIPERAZINE DERIVATIVES
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, (2019/06/30)
The present invention relates to novel compounds of formula (I) or formula (Ia) pharmaceutically-acceptable salts, hydrates, solvates, or stereoisomers thereof, and pharmaceutical compositions of these compounds which are useful for preventive and therapeutic use in human and veterinary medicine.