Zobrazeno 1 - 10
of 44
pro vyhledávání: '"Carmela Molinaro"'
Autor:
Peter E. Maligres, Jeff Fritzen, Guy R. Humphrey, Yonggang Chen, Zhiguo Jake Song, Jonathan E. Wilson, Carmela Molinaro
Publikováno v:
Organic Process Research & Development. 23:2354-2361
2-(2H-Tetrazol-2-yl)benzoic acid 1 and analogs were prepared via Cu(I) catalyzed C–N coupling of 2-iodo or 2-bromo benzoic acids with 5-(ethylthio)-1H-tetrazole followed by reductive cleavage of the thioether bond. The C–N coupling was regioselec
Autor:
Carmela Molinaro, Petronijevic Filip, Francis Gosselin, Sarah J. Robinson, Ngiap-Kie Lim, Theresa Cravillion, Chong Han, C. Gregory Sowell, Xin Linghu, Kelly Sean M, Hong Allen, Nicholas Wong, Haiyun Hou
Publikováno v:
Organic letters. 21(22)
We report herein an efficient, stereocontrolled, and chromatography-free synthesis of the novel broad spectrum antibiotic GDC-5338. The route features the construction of a functionalized tripeptide backbone, a high-yielding macrocyclization via a Pd
Autor:
Baoqiang Wan, Scott Hoerrner, Jaume Balsells, Lu Chen, Bangping Xiang, Qinghao Chen, Lushi Tan, Carmela Molinaro, Eric M. Phillips, Zhongbo Fei, Jingjun Yin, Scott S. Ceglia, Ji Qi, Jiahui Chen, Michael Shevlin, Manuel de Lera Ruiz, Erika M. Milczek
Publikováno v:
The Journal of organic chemistry. 84(12)
A practical and efficient enantioselective synthesis of the calcitonin gene-related peptide receptor antagonist 1 has been developed. The key structural component of the active pharmaceutical ingredient is a syn-1,2-amino-fluoropiperidine 4. Two appr
Autor:
Carmela Molinaro, Ellyn M. Junker, Alain Menard, Jeremy P. Scott, Andrew D. Gibb, Christopher Wise, Michael Shevlin, David R. Lieberman
Publikováno v:
Journal of the American Chemical Society. 137:999-1006
We report a concise, enantio- and diastereoselective route to novel nonsymmetrically substituted N-protected β,β-diaryl-α-amino acids and esters, through the asymmetric hydrogenation of tetrasubstituted olefins, some of the most challenging exampl
Autor:
Sandro Cacchi, Carmela Molinaro, Antonella Goggiamani, Giancarlo Fabrizi, Rosanna Verdiglione
Publikováno v:
The Journal of Organic Chemistry. 79:401-407
A novel palladium-catalyzed approach to 2-(aminomethyl)indoles from 3-(o-trifluoroacetamidoaryl)-1-propargylic alcohols and amines has been developed.
Autor:
Lu Chen, Carmela Molinaro, Qinghao Chen, Yanke Xu, Azzeddine Lekhal, Sarah K. Pulicare, David A. Thaisrivongs, Wenyong Chen, Steven P. Miller, Zhiguo J. Song, Lushi Tan
Publikováno v:
Organic letters. 18(22)
Verubecestat is an inhibitor of β-secretase being evaluated for the treatment of Alzheimer’s disease. The first-generation route relies on an amide coupling with a functionalized aniline, the preparation of which introduces synthetic inefficiencie
Autor:
Li Hao, Carolyn Bahnck-Teets, Catherine M. Wiscount, Daniel J. McKay, Carmela Molinaro, Ronald K. Chang, S S Carroll, Sivalenka Vijayasaradhi, Philippe G. Nantermet, Sanjay Kumar Singh, Christopher J. Bungard, Dubost David C, David Jonathan Bennett, Thomas J. Greshock, Hua-Poo Su, Rosa I. Sanchez, Vouy Linh Truong, Xu Min, John F. Fay, Jeanine E. Ballard, John A. McCauley, Christian Beaulieu, M. Katharine Holloway, Joseph P. Vacca, Michael W. Miller, Tummanapalli Satyanarayana, Sheldon Crane, William D. Shipe, Jesse J. Manikowski, Peter D. Williams, Christian Nadeau, Jennifer J. Gesell, Tracy L. Diamond, Peter J. Felock, Oscar Miguel Moradei
A novel HIV protease inhibitor was designed using a morpholine core as the aspartate binding group. Analysis of the crystal structure of the initial lead bound to HIV protease enabled optimization of enzyme potency and antiviral activity. This afford
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::82f685aed82b9b428b5b9e7330d8f427
https://europepmc.org/articles/PMC4948015/
https://europepmc.org/articles/PMC4948015/
Autor:
Debra J. Wallace, Paul D. O’Shea, Carmela Molinaro, Paul G. Bulger, Stephen Lau, Melissa E. Howard, Danny Gauvreau, Birgit Kosjek, Ernest E. Lee
Publikováno v:
The Journal of Organic Chemistry. 77:2299-2309
In this paper, we report the development of different synthetic routes to MK-7246 (1) designed by the Process Chemistry group. The syntheses were initially designed as an enabling tool for Medicinal Chemistry colleagues in order to rapidly explore st
Autor:
Robert Houle, Jean François Lévesque, Daniel Simard, François G. Gervais, Carl Berthelette, Carmela Molinaro, Yves Leblanc, Martine Hamel, Michel Gallant, Helmi Zaghdane, Nicole Sawyer, Susan Sillaots, Zhaoyin Wang, Michael J. Boyd, John Colucci, Rino Stocco
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3471-3474
A new series of indole amide acting as hCRTH2 receptor ligands had been explored and are described herein. Several amide derivatives displaying low nanomolar activity in hCRTH2 binding and whole blood assays were identified. They were found to behave
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