Results 41 to 50 of about 47,089 (385)

A Versatile Class of 1,4,4-Trisubstituted Piperidines Block Coronavirus Replication In Vitro

Pharmaceuticals, 2022
There is a clear need for novel antiviral concepts to control SARS-CoV-2 infection. Based on the promising anti-coronavirus activity observed for a class of 1,4,4-trisubstituted piperidines, we here conducted a detailed analysis of the structure–activity
Sonia De Castro, Annelies Stevaert, Miguel Maldonado, Adrien Delpal, Julie Vandeput, Benjamin Van Loy, Cecilia Eydoux, Jean-Claude Guillemot, Etienne Decroly, Federico Gago, Bruno Canard, Maria-Jose Camarasa, Sonsoles Velázquez, Lieve Naesens   +13 more
doaj   +1 more source

Frontispiece: A Pd-Catalyzed Synthesis of Functionalized Piperidines [PDF]

, 2016
Pd Catalysis A readily available cyclic carbamate functions as a general precursor to a range of functionalized piperidine products using a new Pd-catalyzed annulation strategy.
Allen, B.D.W., Connolly, M.J., Harrity, J.P.A.   +2 more
core   +1 more source

Synthesis of Novel IP Agonists via N-Aminoethyl Cyclic Amines Prepared by Decarboxylative Ring-Opening Reactions

Molecules, 2012
An efficient synthesis of a highly potent and selective IP (PGI2 receptor) agonist that is not structurally analogous to PGI2 is described. This synthesis is accomplished through the following key steps: Nucleophilic ring-opening of 3-(4-chlorophenyl ...
Masashi Uchida, Mitsuko Miyamoto, Mika Kitsukawa, Masafumi Isogaya, Ryoji Hayashi, Kuniaki Kawamura, Takeshi Ishigaki, Yasuhiro Morita, Katsuhiko Iseki   +8 more
doaj   +1 more source

Modular synthesis of chiral 1,2-dihydropyridines via Mannich/Wittig/cycloisomerization sequence that internally reuses waste

Nature Communications, 2021
1,2-Dihydropyridines are valuable precursors for the synthesis of biologically relevant piperidines and pyridines, but the methods for their synthesis are underdeveloped.
Bo-Shuai Mu, Xiao-Yuan Cui, Xing-Ping Zeng, Jin-Sheng Yu, Jian Zhou   +4 more
doaj   +1 more source

Chiral piperidines from acyclic amines via enantioselective, radical-mediated δ C-H cyanation.

Chem, 2019
Piperidines are the most prevalent heterocycle found in medicines. Yet, while they are often chiral, there remain no robust methods for their asymmetric syntheses. To solve this challenge, we have interrupted the century-old Hofmann-Löffler-Freytag (HLF)
Zuxiao Zhang, Xin Zhang, David A. Nagib
semanticscholar   +1 more source

Synthesis of Nitrogenated Heterocycles by Asymmetric Transfer Hydrogenation of N-(tert-Butylsulfinyl)haloimines [PDF]

, 2013
Highly optically enriched, protected, nitrogenated heterocycles with different ring sizes have been synthesized by a very efficient methodology consisting of the asymmetric transfer hydrogenation of N-(tert-butylsulfinyl)haloimines followed by treatment ...
Ahn K., Almansa R., Almansa R., Alonso D. A., Andersson P. G., Bañón-Caballero A., Bosque I., Brak K., Breuer M., Callebaut G., Collados J. F., Corey E. J., Cutter A. C., Daly J. W., Darwish M., David Guijarro, Dema H. K., Denolf B., Denolf B., Dua R., Elliott R. L., Ellman J. A., Ellman J. A., Fattorusso E., Ferreira F., Gowda M., Guijarro D., Guijarro D., Guijarro D., Guijarro D., Guijarro D., Guijarro D., Guo T., Hansen K. B., Hart H., Hodgson D. M., Hodgson D. M., Holzer M., Kobayashi S., Kosciolowicz A., Lawrence A. K., Leemans E., Leemans E., Lin G.-Q., Lin N.-H., Louvel J., Louvel J., Mao J., Melchiorre P., Michael J. P., Miguel Yus, Noyori R., Nugent T. C., Nájera C., O’Hagan D., Pablo O., Palmer M. J., Patil M. P., Pinho P., Rao M. L. N., Reddy L. R., Reddy L. R., Reddy L. R., Robak M. T., Roth P., Royer J., Samano V., Senanayake C. H., Senter T. J., Siva S. R. N., Sun X., Tanner D., Vaultier M., Voituriez A., Wang C., Yu J., Óscar Pablo   +76 more
core   +2 more sources

Catalytic asymmetric synthesis of the alkaloid (+)-myrtine [PDF]

, 2008
A new protocol for the asymmetric synthesis of trans-2,6-disubstituted-4-piperidones has been developed using a catalytic enantioselective conjugate addition reaction in combination with a diastereoselective lithiation–substitution sequence; an efficient
Adriaan J. Minnaard, Albrow, Alexakis, Alexakis, Anderson, Bach, Back, Beak, Beak, Beak, Beak, Beak, Beak, Beak, Ben L. Feringa, Bennett, Bennett, Berkheij, Bertini Gross, Brooks, Comins, Comins, Comins, Comins, Comins, Comins, Comins, Curtin, d'Augustin, Davis, Dieter, Dieter, Dieter, Dieter, Dieter, Eilitz, Frankel, Fraser, Gallagher, Garcia-Ruiz, Gardette, Gelas-Mialhe, Hoffmann, Houk, Kerrick, King, Leclercq, Liang, Maria Gabriella Pizzuti, Pilli, Pilli, Pineschi, Pàmies, Remuson, Slosse, Slosse, Still, Tawara, Vuagnoux-d'Augustin, Vuagnoux-d'Augustin, Watson, Whisler, Šebesta   +62 more
core   +1 more source

Copper(I)-Catalyzed Cross-Coupling of 1-Bromoalkynes with N-Heterocyclic Organozinc Reagents

Molecules, 2022
Nitrogen-containing heterocycles represent the majority of FDA-approved small-molecule pharmaceuticals. Herein, we describe a synthetic method to produce saturated N-heterocyclic drug scaffolds with an internal alkyne for elaboration.
Christian Frabitore, Jérome Lépeule, Tom Livinghouse   +2 more
doaj   +1 more source

First selective direct mono-arylation of piperidines using ruthenium-catalyzed C–H activation [PDF]

, 2013
: A Ru-catalyzed mono-arylation in α-position of saturated cyclic amines is reported employing a C–H activation protocol. Substitution of the pyridine directing group with a bulky group, e.g., trifluoromethyl in the 3-position, proved to be crucial to ...
Karl Kirchner, Maria C. Schwarz, Marko D. Mihovilovic, Michael Schnürch, Navid Dastbaravardeh   +4 more
core   +1 more source

Electrochemical Aminoxyl-Mediated α-Cyanation of Secondary Piperidines for Pharmaceutical Building Block Diversification.

Journal of the American Chemical Society, 2018
Secondary piperidines are ideal pharmaceutical building blocks owing to the prevalence of piperidines in commercial drugs. Here, we report an electrochemical method for cyanation of the heterocycle adjacent to nitrogen without requiring protection or ...
A. Lennox, Shannon L. Goes, Matthew P. Webster, H. Koolman, S. Djuric, S. Stahl   +5 more
semanticscholar   +1 more source