Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Stéphane G. Ouellet"'
Autor:
Paul D. O’Shea, Louis-Charles Campeau, Stéphane G. Ouellet, Mélina Girardin, Paul N. Devine, Danny Gauvreau, Jeffrey C. Moore, Greg Hughes
Publikováno v:
Organic Process Research & Development. 17:61-68
MK-6096 is an orexin receptor antagonist in clinical trials for the treatment of insomnia. Herein we describe its first kilogram-scale synthesis. Chirality on the α-methylpiperidine core was introduced in a biocatalytic transamination using a three-
Autor:
Greg Hughes, Ian W. Davies, Louis-Charles Campeau, Danny Gauvreau, Paul D. O’Shea, Sarah J. Dolman, Mark Cameron, Stéphane G. Ouellet
Publikováno v:
Organic Process Research & Development. 16:214-219
Process research and development of a synthetic route towards a novel 5-lipoxygenase inhibitor is described. The synthetic route provided 1 in 27% yield in nine steps (seven steps in the longest linear sequence) and was performed on kilogram scale. T
Autor:
Paul Fernandez, Sarah J. Dolman, Stéphane G. Ouellet, George Zhou, Greg Hughes, Paul D. O’Shea, Sophie Lauzon, Mélina Girardin
Publikováno v:
Organic Process Research & Development. 15:1073-1080
A practical kilogram scale chromatography-free synthesis of stearoyl-CoA desaturase 1 (SCD1) inhibitor MK-8245 is described. The key features of this sequence include an efficient addition–eliminat...
Autor:
Jinchu Liu, Dietrich Steinhuebel, Mark Weisel, Erin N. Guidry, Ed Corley, Paul D. O’Shea, Louis-Charles Campeau, Stéphane G. Ouellet, Danny Gauvreau, Sarah J. Dolman
Publikováno v:
Organic Process Research & Development. 15:1138-1148
Process research and development of a synthetic route towards a novel renin inhibitor (1) is described. The highly convergent synthetic route provided 1 in 15% yield on multikilogram scale with a longest linear sequence of 11 steps. The use of cataly
Autor:
Carmela Molinaro, Ian W. Davies, Jean-François Marcoux, Stéphane G. Ouellet, Amélie Roy, Remy Angelaud, Paul D. O’Shea
Publikováno v:
The Journal of Organic Chemistry. 76:1436-1439
In this report, we disclose our findings regarding the remarkable effect of a low-level impurity found in the solvent used for a ruthenium-catalyzed direct arylation reaction. This discovery allowed for the development of a robust and high-yield aryl
Publikováno v:
Tetrahedron Letters. 50:3776-3779
In this Letter, we describe a practical and highly selective method for the preparation of fluoroaryl ethers and differentially substituted resorcinol derivatives. This synthetic strategy relies on a selective SNAr of substituted difluorobenzene deri
Autor:
Sarah J. Dolman, Pamela G. Alsabeh, Greg Hughes, Mélina Girardin, Stéphane G. Ouellet, Sophie Lauzon
Publikováno v:
Organic Letters. 11:1159-1162
A novel two-step procedure for the synthesis of 3-amino-5-substituted-isoxazoles is described. In the presence of a base, readily available 3-bromoisoxazolines react with amines to afford 3-aminoisoxazolines. An oxidation protocol was developed for t
Autor:
Rico Lavoie, Yves L. Dory, Stéphane G. Ouellet, Carol Dallaire, Pierre Deslongchamps, András Toró
Publikováno v:
Tetrahedron. 56:5509-5522
Highly convergent, malonate alkylation based syntheses of the model macrocycles and their title investigations are reported. In the allylic ether dienophile case, a preference for tricycles with equatorial ether position was found at the transition s
Autor:
Nguyen Natalie, Ernest Asante-Appiah, Manuel Chan, Nathalie Coulombe, Yves Ducharme, Mark Wrona, C. Bayly, Paul Tawa, Serge Plamondon, Kristina Dupont-Gaudet, Amandine Chefson, Jean-François Truchon, Sébastien Guiral, Louis-Charles Campeau, Joe Vacca, Sébastien Gagné, Rob Papp, Elizabeth Cauchon, Leanne Bedard, Eric Langlois, Robert Forget, Stéphane G. Ouellet, Stephanie Roy, Mélina Girardin, Jason Burch, Jean-Pierre Falgueyret, Bernard Cote, Danny Gauvreau, St-Onge Miguel, Marc Blouin, Ria Seliniotakis, Wanda Cromlish, Chun Sing Li, Amélie Roy, Smita Debnath, Youwei Yan, Denis Deschenes
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(3)
The optimization of a novel series of non-nucleoside reverse transcriptase inhibitors (NNRTI) led to the identification of pyridone 36. In cell cultures, this new NNRTI shows a superior potency profile against a range of wild type and clinically rele
Autor:
David A. Powell, Geoffrey K. Tranmer, Nicolas Lachance, Zheng Huang, Yeeman K. Ramtohul, Stéphane G. Ouellet, Thao Trinh, Lei Zhang, Serge Leger, Hao Wang, Jean-Philippe Leclerc, Elise Isabel, Yves Gareau, Christian Nadeau, Evelyn Martins, Sébastien Guiral, Renata Oballa
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(2)
Inhibition of stearoyl-CoA desaturase (SCD) activity represents a potential novel mechanism for the treatment of metabolic disorders including obesity and type II diabetes. To circumvent skin and eye adverse events observed in rodents with systemical