Search Results - "Humphrey, Guy"

Practical Methodologies for the Synthesis of Indoles by Humphrey, Guy R, Kuethe, Jeffrey T

“…A review of practical methodologies for the synthesis of indoles is presented. The indole ring system is probably the most ubiquitous heterocycle in nature…”
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The Emergence of Universal Chromatographic Methods in the Research and Development of New Drug Substances by Regalado, Erik L, Haidar Ahmad, Imad A, Bennett, Raffeal, D’Atri, Valentina, Makarov, Alexey A, Humphrey, Guy R, Mangion, Ian, Guillarme, Davy

“…Conspectus Manufacturing process development of new drug substances in the pharmaceutical industry combines numerous chemical challenges beyond the efficient…”
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Harnessing the Power of Catalysis for the Synthesis of CRTH2 Antagonist MK-1029 by Ruck, Rebecca T, Pan, Jun, Vaswani, Rishi G, Kosjek, Birgit, Strotman, Neil A, Cai, Chaoxian, Humphrey, Guy R

“…The synthetic strategy utilized to prepare clinical supplies of CRTH2 antagonist MK-1029 is described. Specifically, the approach communicated is predicated on…”
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Process Development of C–N Cross-Coupling and Enantioselective Biocatalytic Reactions for the Asymmetric Synthesis of Niraparib by Chung, Cheol K, Bulger, Paul G, Kosjek, Birgit, Belyk, Kevin M, Rivera, Nelo, Scott, Mark E, Humphrey, Guy R, Limanto, John, Bachert, Donald C, Emerson, Khateeta M

“…Process development of the synthesis of the orally active poly(ADP-ribose)polymerase inhibitor niraparib is described. Two new asymmetric routes are reported,…”
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Asymmetric Hydrogen Bonding Catalysis for the Synthesis of Dihydroquinazoline-Containing Antiviral, Letermovir by Chung, Cheol K, Liu, Zhijian, Lexa, Katrina W, Andreani, Teresa, Xu, Yingju, Ji, Yining, DiRocco, Daniel A, Humphrey, Guy R, Ruck, Rebecca T

“…A weak Brønsted acid-catalyzed asymmetric guanidine aza-conjugate addition reaction has been developed. C2-symmetric, dual hydrogen-bond donating…”
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Development of a Robust Manufacturing Route for Molnupiravir, an Antiviral for the Treatment of COVID-19 by Fier, Patrick S., Xu, Yingju, Poirier, Marc, Brito, Gilmar, Zheng, Michelle, Bade, Rachel, Sirota, Eric, Stone, Kevin, Tan, Lushi, Humphrey, Guy R., Chang, Darryl, Bothe, Jameson, Zhang, Yongqian, Bernardoni, Frank, Castro, Steve, Zompa, Michael A., Taylor, Jerry, Sirk, Kevin M., Diaz-Santana, Anthony, Diribe, Ike, Emerson, Khateeta M., Krishnamurthi, Bharath, Zhao, Ralph, Ward, Michael, Xiao, Chengqian, Ouyand, Honggui, Zhan, Jianfeng, Morris, William J.

“…Herein is described the development of a large-scale manufacturing process for molnupiravir, an orally dosed antiviral that was recently demonstrated to be…”
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Development of a Commercial Manufacturing Route to 2‑Fluoroadenine, The Key Unnatural Nucleobase of Islatravir by Hong, Cynthia M, Xu, Yingju, Chung, John Y. L, Schultz, Danielle M, Weisel, Mark, Varsolona, Richard J, Zhong, Yong-Li, Purohit, Akasha K, He, Cyndi Q, Gauthier, Donald R, Humphrey, Guy R, Maloney, Kevin M, Lévesque, François, Wang, Zhixun, Whittaker, Aaron M, Sirota, Eric, McMullen, Jonathan P

“…We report the practical synthesis of a key fragment of islatravir (MK-8591), a novel nucleoside reverse transcriptase translocation inhibitor (NRTTI) currently…”
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Development of a Novel, Highly Efficient Halide-Catalyzed Sulfenylation of Indoles by Tudge, Matthew, Tamiya, Minoru, Savarin, Cecile, Humphrey, Guy R

“…The reaction of a variety of indoles with N-thioalkyl- and N-thioarylphthalimides to produce 3-thioindoles is reported. Catalytic quantities of…”
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A Green Chemistry Continuum for a Robust and Sustainable Active Pharmaceutical Ingredient Supply Chain by Koenig, Stefan G, Bee, Cisco, Borovika, Alina, Briddell, Christiana, Colberg, Juan, Humphrey, Guy R, Kopach, Michael E, Martinez, Isamir, Nambiar, Sudhir, Plummer, Scott V, Ribe, Seth D, Roschangar, Frank, Scott, Jeremy P, Sneddon, Helen F

“…In an effort to improve sustainability and reduce the cost of goods for active pharmaceutical ingredients (APIs), pharma companies have partnered on varying…”
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Combining traditional 2D and modern physical organic-derived descriptors to predict enhanced enantioselectivity for the key aza-Michael conjugate addition in the synthesis of Prevymis™ (letermovir) by Metsänen, Toni T, Lexa, Katrina W, Santiago, Celine B, Chung, Cheol K, Xu, Yingju, Liu, Zhijian, Humphrey, Guy R, Ruck, Rebecca T, Sherer, Edward C, Sigman, Matthew S

“…Quantitative structure-activity relationships have an extensive history for optimizing drug candidates, yet they have only recently been applied in reaction…”
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Asymmetric Synthesis of Telcagepant, a CGRP Receptor Antagonist for the Treatment of Migraine by Xu, Feng, Zacuto, Michael, Yoshikawa, Naoki, Desmond, Richard, Hoerrner, Scott, Itoh, Tetsuji, Journet, Michel, Humphrey, Guy R, Cowden, Cameron, Strotman, Neil, Devine, Paul

“…A highly efficient, asymmetric synthesis of telcagepant (1), a CGRP receptor antagonist for the treatment of migraine, is described. This synthesis features…”
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Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 2: Development of a Robust Process for Phenol Synthesis by Peng, Feng, Humphrey, Guy R, Maloney, Kevin M, Lehnherr, Dan, Weisel, Mark, Lévesque, Francois, Naber, John R, Brunskill, Andrew P. J, Larpent, Patrick, Zhang, Si-Wei, Lee, Alfred Y, Arvary, Rebecca A, Lee, Claire H, Bishara, Daniel, Narsimhan, Karthik, Sirota, Eric, Whittington, Michael

“…Various synthetic routes to 2-isopropyl-4-methoxyphenol 3, the phenol core of Gefapixant citrate (MK-7264), are described, which provide better alternatives to…”
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Asymmetric Synthesis of a Potent HIV‑1 Integrase Inhibitor by Kuethe, Jeffrey T, Humphrey, Guy R, Journet, Michel, Peng, Zhihui, Childers, Karla G

“…The development of a practical asymmetric total synthesis of the potent HIV-1 integrase inhibitor 5 is described. Key transformations include construction of…”
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Asymmetric Synthesis of Functionalized trans-Cyclopropoxy Building Block for Grazoprevir by Xu, Feng, Zhong, Yong-Li, Li, Hongming, Qi, Ji, Desmond, Richard, Song, Zhiguo J, Park, Jeonghan, Wang, Tao, Truppo, Matthew, Humphrey, Guy R, Ruck, Rebecca T

“…A practical and asymmetric synthesis of a functionalized trans-cyclopropoxy building block for the preparation of the HCV NS3/4a protease inhibitor grazoprevir…”
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Development of a Scalable and Safer Synthesis of Diazeniumdiolates by Zhong, Yong-Li, Muzzio, Daniel J, Weisel, Mark, Zhang, Li, Humphrey, Guy R, Maloney, Kevin M, Campos, Kevin R

“…Although diazeniumdiolates (DAZDs) and the synthetic methods to access DAZDs were discovered over 50 years ago, the current methodology is not safe, has a…”
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Highly Efficient Synthesis of HIV NNRTI Doravirine by Gauthier, Donald R, Sherry, Benjamin D, Cao, Yang, Journet, Michel, Humphrey, Guy, Itoh, Tetsuji, Mangion, Ian, Tschaen, David M

“…The development of an efficient and robust process for the production of HIV NNRTI doravirine is described. The synthesis features a continuous aldol reaction…”
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Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 1: Introduction and Process Overview by Ren, Hong, Maloney, Kevin M, Basu, Kallol, Di Maso, Michael J, Humphrey, Guy R, Peng, Feng, Desmond, Richard, Otte, Douglas A. L, Alwedi, Embarek, Liu, Wenjun, Zhang, Si-Wei, Song, Siqing, Arvary, Rebecca A, Zompa, Michael A, Lehnherr, Dan, Martin, Gary E, Chang, Hsieh Yao D, Mohan, Anne E, Guzman, Francisco J, Jellett, Lisa, Lee, Alfred Y, Spencer, Glenn, Fisher, Elizabeth S, Naber, John R, Gao, Hong, Lohani, Sachin, Ruck, Rebecca T, Campeau, Louis-Charles

“…A robust, green, and sustainable manufacturing process has been developed for the synthesis of gefapixant citrate, a P2X3 receptor antagonist that is under…”
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Scalable Synthesis of Diazeniumdiolates: Application to the Preparation of MK-8150 by Zhong, Yong-Li, Weisel, Mark, Humphrey, Guy R, Muzzio, Daniel J, Zhang, Li, Huffman, Mark A, Zhong, Wendy, Maloney, Kevin M, Campos, Kevin R

“…Synthetic diazeniumdiolate (DAZD)-based nitric oxide is utilized to modulate the nitric oxide (NO) concentration in cellular environments and to control…”
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Development of a Multikilogram Scale Synthesis of a TRPV1 Antagonist by Kuethe, Jeffrey T, Journet, Michel, Peng, Zhihui, Zhao, Dalian, McKeown, Arlene, Humphrey, Guy R

“…A highly efficient, regioselective five-step synthesis of the TRPV1 antagonist 1 is described. The coupling of piperazine 7 with dichloropyrimidine 8 proceeded…”
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Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264). Part 6: Development of an Improved Commercial Salt Formation Process by Maloney, Kevin M, Zhang, Si-Wei, Mohan, Anne E, Lee, Alfred Y, Larpent, Patrick, Ren, Hong, Humphrey, Guy R, Desmond, Richard, DiBenedetto, Michael, Liu, Wenjun, Lee, Ivan H, Sirota, Eric, Di Maso, Michael J, Alwedi, Embarek, Song, Siqing, Chang, Hsieh Yao D

“…The development of a sustainable commercial salt formation process for gefapixant citrate (MK-7264), an investigational new P2X3 antagonist for the treatment…”
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