Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Pablo Garcia-Losada"'
Autor:
Carlos Mateos, Juan A. Rincón, Michael O. Frederick, Timothy Noël, Pablo Garcia-Losada, Gabriele Laudadio, Ting Wan, Luca Capaldo, Alexander V. Nyuchev, Manuel Nuño
Publikováno v:
Angewandte Chemie, 133(33), 18037-18041. John Wiley and Sons Ltd
Angewandte Chemie, International Edition, 60(33), 17893-17897. John Wiley and Sons Ltd
Angewandte Chemie International Edition
Angewandte Chemie, International Edition, 60(33), 17893-17897. John Wiley and Sons Ltd
Angewandte Chemie International Edition
Photocatalytic hydrogen atom transfer is a very powerful strategy for the regioselective C(sp3)-H functionalization of organic molecules. Herein, we report on the unprecedented combination of decatungstate hydrogen atom transfer photocatalysis with t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b82f9236e996f407460e7980499888dc
https://doi.org/10.1002/ange.202104682
https://doi.org/10.1002/ange.202104682
Autor:
Hao Sun, Michael O. Frederick, Roger Ryan Rothhaar, Amy C. DeBaillie, Brian Morgan Watson, Carlos Mateos, Leonard L. Winneroski, Carlos Jaramillo, Talbi Kaoudi, Matthew Johnson, Pablo Garcia-Losada, Srinivas Gangula, Peter J. Lindsay-Scott, Steven James Green, Dustin J. Mergott, Dajiang Jing, Marvin M. Hansen, José Eugenio de Diego, Juan A. Rincón, Kevin D. Seibert, Lei Zhang, Jiuyuan Li
Publikováno v:
Organic Process Research & Development. 24:306-314
Herein we report a summary of the synthetic development of LY3202626 from the initial discovery route to a final route that was scaled to make 150 kg. Key developments include the use of a [3 + 2] ...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bd409beaf54c99668ae6510bc63b7fdb
https://doi.org/10.1021/acs.oprd.9b00471
https://doi.org/10.1021/acs.oprd.9b00471
Autor:
Stephanie L. Stout, Leonard L. Winneroski, Jorg Hendle, Warren J. Porter, Patrick J. C. May, Leonard N. Boggs, Thomas K. Baker, James P. Beck, Steven James Green, Anthony R. Borders, Erik James Hembre, Stephen L. Lowe, Christopher D Aluise, David L. McKinzie, Brian Morgan Watson, Brian Michael Mathes, Jon A. Erickson, Zhixiang Yang, Patrick J Cocke, Dustin J. Mergott, Brian A. Willis, Scott A. Monk, Pablo Garcia-Losada, David E. Timm, Richard A. Brier, Jose Eduardo Lopez
Publikováno v:
Journal of medicinal chemistry. 64(12)
The beta-site APP cleaving enzyme 1, known as BACE1, has been a widely pursued Alzheimer's disease drug target owing to its critical role in the production of amyloid-beta. We have previously reported the clinical development of LY2811376 and LY28867
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::698057ee408d2f35c662510d099e51b3
https://pubmed.ncbi.nlm.nih.gov/34081466
https://pubmed.ncbi.nlm.nih.gov/34081466
Autor:
Andrew D. Campbell, Rubén Haro, Thomas Andrew Brandt, Melodie Christensen, David B. Damon, Ke Wang, Carolina Alhambra, Paul C. Lobben, Jacob M. Janey, J. Eugenio de Diego, Ling Li, Iulia I. Strambeanu, Susana García-Cerrada, Javier Magano, Emma McInturff, Steven M. Mennen, Jack Twilton, David W. C. MacMillan, Fangfang Liu, Jesús Castañón, Matthew A. Zajac, Pablo Garcia-Losada, Sebastien Monfette, Mario Barberis, Alan H. Cherney, Jason M. Stevens, Barbara J. Sitter, Danielle M. Schultz, Ronald J. Post, Simon Berritt, C. Liana Allen, David C. Leitch
Publikováno v:
Organic Process Research & Development. 23:1213-1242
High-throughput experimentation (HTE) has revolutionized the pharmaceutical industry, most notably allowing for rapid screening of compound libraries against therapeutic targets. The past decade ha...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7d057d4265eaefcd550f067f2a336489
https://doi.org/10.1021/acs.oprd.9b00140
https://doi.org/10.1021/acs.oprd.9b00140
Autor:
Myriam Torres, Pablo Garcia-Losada, Juan A. Rincón, María Ruiz-Abad, María José Nieves-Remacha, Graham R. Cumming
Publikováno v:
Reaction Chemistry & Engineering. 4:334-345
A continuous phase-transfer catalysis process for N-alkylation integrated with separation was developed. This approach circumvents the heat and mass transfer limitations encountered in batch scale-up, enabling a safer process and yielding a higher-qu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6bed637f467b20913fb0c485e04f3786
https://doi.org/10.1039/c8re00203g
https://doi.org/10.1039/c8re00203g
Autor:
Leonard L. Winneroski, Dustin J. Mergott, Amy C. DeBaillie, Yuan Shi, Brian Morgan Watson, Francisco Martínez-Olid, Carolina Alhambra Jimenez, Mario Barberis, Chauncey D. Jones, Pablo Garcia-Losada, Erik James Hembre
Publikováno v:
Organic Process Research & Development. 22:650-654
Here we report an optimized protocol for the asymmetric introduction of a fluorine atom into a quaternary center facilitated by d-proline, Selectfluor®, and trifluoroethanol. The synthesis proceeds over four steps starting from a chiral amino alcoho
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::605c2844dfb8d56a6a2a8fae33d2b3e2
https://doi.org/10.1021/acs.oprd.8b00069
https://doi.org/10.1021/acs.oprd.8b00069
Autor:
Susana García-Cerrada, Pablo Garcia-Losada, Juan A. Rincón, Francisco Martínez-Olid, Laura Redondo-Gallego
Publikováno v:
Organic Process Research & Development. 21:779-784
The diastereoselective preparation of cis- or trans-4-substituted-4-aminocyclohexyl alcohols by conventional chemical processes reported in the literature requires long synthetic sequences and is not amenable to scale-up. In the past decade, ketoredu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::76511b206b49190a21d3fa461a959b01
https://doi.org/10.1021/acs.oprd.7b00048
https://doi.org/10.1021/acs.oprd.7b00048
Autor:
Kostas Gavardinas, John G. Luz, Nathan A. Calvert, Vaught Grant Matthews, Pablo Garcia Losada, Heather A Bullock, Ashraf Saeed, Donald P. Matthews, Yong Wang, Nita J. Patel, Venkatesh Krishnan, Judith W. Henck, Jonathan Edward Green, Sweetana Stephanie Ann, Prabhakar Kondaji Jadhav
Publikováno v:
Journal of Medicinal Chemistry. 59:750-755
A transdermal SARM has a potential to have therapeutic benefit through anabolic activity in muscle while sparing undesired effects of benign prostate hyperplasia (BPH) and liver-mediated decrease in HDL-C. 2-Chloro-4-[(2-hydroxy-2-methyl-cyclopentyl)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72fb49ad5057da8c107176f52e98ce6e
https://doi.org/10.1021/acs.jmedchem.5b01168
https://doi.org/10.1021/acs.jmedchem.5b01168
Autor:
David E. Timm, Leonard N. Boggs, Brian Michael Mathes, Yuan Shi, Mario Barberis, Zhixiang Yang, Dustin J. Mergott, Scott A. Monk, Pablo Garcia-Losada, Jose Miguel Minguez, Leonard L. Winneroski, Jon A. Erickson, Richard A. Brier, Anthony R. Borders, Stephanie L. Stout, Porter Warren J, Zoran Rankovic, Jose Eduardo Lopez, Erik James Hembre, James E. Audia, Jorg Hendle, James P. Beck, Steven James Green, Brian Morgan Watson, Patrick C. May, Robert D. Boyer
Publikováno v:
Bioorganic & Medicinal Chemistry. 28:115194
Inhibition of BACE1 has become an important strategy in the quest for disease modifying agents to slow the progression of Alzheimer's disease. We previously reported the fragment-based discovery of LY2811376, the first BACE1 inhibitor reported to dem
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::686975880a947f8f81325a11d876e66b
https://doi.org/10.1016/j.bmc.2019.115194
https://doi.org/10.1016/j.bmc.2019.115194
Publikováno v:
Organic Process Research & Development. 19:347-351
Here, we report a continuous flow protocol for the [3 + 2] cycloaddition of nitrones, in situ generated from oximes, into bicyclic isoxazolidines. This thermal process required very high temperatures to be efficient that were not easily reached in co
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6978b3276ca641355761ffd76b06efaa
https://doi.org/10.1021/op500350y
https://doi.org/10.1021/op500350y