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Autor:
Matthew S. Winston, Marc Poirier, Zhijian Liu, Feng Peng, Guy R. Humphrey, John A. McIntosh, Mikhail Reibarkh, Fengqiang Wang, Erik D. Guetschow, Steve Castro, Erik Hoyt, David J. Lamberto, Kevin Sirk
Publikováno v:
Organic Process Research & Development. 27:179-188
Autor:
Birgit Kosjek, Rishi G. Vaswani, Neil A. Strotman, Jun Pan, Chaoxian Cai, Rebecca T. Ruck, Guy R. Humphrey
Publikováno v:
Organic Process Research & Development. 26:648-656
Autor:
Anne E. Mohan, Siqing Song, Hsieh Yao D. Chang, Si-Wei Zhang, Patrick Larpent, Wenjun Liu, Michael DiBenedetto, Eric B. Sirota, Michael J. Di Maso, Richard Desmond, Kevin M. Maloney, Ivan H. Lee, Alfred Y. Lee, Guy R. Humphrey, Embarek Alwedi, Hong Ren
Publikováno v:
Organic Process Research & Development. 24:2498-2504
The development of a sustainable commercial salt formation process for gefapixant citrate (MK-7264), an investigational new P2X3 antagonist for the treatment of chronic cough, is described. Due to ...
Autor:
Eric B. Sirota, Karthik Narsimhan, Feng Peng, Mark Weisel, Alfred Y. Lee, Rebecca A. Arvary, Claire Lee, Daniel Bishara, Kevin M. Maloney, Andrew Brunskill, François Lévesque, Patrick Larpent, Michael Whittington, John R. Naber, Guy R. Humphrey, Dan Lehnherr, Si-Wei Zhang
Publikováno v:
Organic Process Research & Development. 24:2453-2461
Various synthetic routes to 2-isopropyl-4-methoxyphenol 3, the phenol core of Gefapixant citrate (MK-7264), are described, which provide better alternatives to the initial four-step supply route. T...
Autor:
Michael J. Di Maso, Embarek Alwedi, Guy R. Humphrey, Richard Desmond, Louis-Charles Campeau, Lisa Jellett, John R. Naber, Hong Ren, Hsieh Yao D. Chang, Douglas A. L. Otte, Hong Gao, Michael A. Zompa, Si-Wei Zhang, Gary E. Martin, Alfred Y. Lee, Wenjun Liu, Francisco J. Guzman, Kevin M. Maloney, Feng Peng, Elizabeth Fisher, Rebecca T. Ruck, Dan Lehnherr, Anne E. Mohan, Glenn Spencer, Siqing Song, Kallol Basu, Rebecca A. Arvary, Sachin Lohani
Publikováno v:
Organic Process Research & Development. 24:2445-2452
A robust, green, and sustainable manufacturing process has been developed for the synthesis of gefapixant citrate, a P2X3 receptor antagonist that is under investigation for the treatment of refrac...
Autor:
Kevin R. Campos, Kevin M. Maloney, Li Zhang, Yong-Li Zhong, Daniel J. Muzzio, Guy R. Humphrey, Mark Weisel
Publikováno v:
Organic Process Research & Development. 24:1602-1608
Although diazeniumdiolates (DAZDs) and the synthetic methods to access DAZDs were discovered over 50 years ago, the current methodology is not safe, has a limited substrate scope, and is not amenab...
Autor:
Zhixun Wang, Eric B. Sirota, Mark Weisel, John Y. L. Chung, Aaron M. Whittaker, Cyndi Qixin He, Donald R. Gauthier, François Lévesque, Danielle M. Schultz, Akasha K. Purohit, Yong-Li Zhong, Yingju Xu, Jonathan P. McMullen, Guy R. Humphrey, Varsolona Richard J, Cynthia M. Hong, Kevin M. Maloney
Publikováno v:
Organic Process Research & Development. 25:395-404
We report the practical synthesis of a key fragment of islatravir (MK-8591), a novel nucleoside reverse transcriptase translocation inhibitor (NRTTI) currently under investigation for treatment and...
Autor:
Peter E. Maligres, Tao Pei, Jinquin Yin, Zhiguo Jake Song, Guy R. Humphrey, Tetsuji Itoh, Hallena R. Strotman, Edward C. Sherer, Neil A. Strotman
Publikováno v:
Synthesis. 52:3378-3388
Controlling the absolute and relative stereochemistry of a seven-membered oxepane in the formation of HIV integrase inhibitor MK-1376 was accomplished through a strategy involving the use of asymmetric allylation and stereoconvergent, substrate-direc
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