Search Results - "Belyk, Kevin"

Discovery and Application of Doubly Quaternized Cinchona-Alkaloid-Based Phase-Transfer Catalysts by Xiang, Bangping, Belyk, Kevin M., Reamer, Robert A., Yasuda, Nobuyoshi

“…We report the discovery of novel N,N′‐disubstituted cinchona alkaloids as efficient phase‐transfer catalysts for the assembly of stereogenic quaternary…”
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Enantioselective Synthesis of N‑Benzylic Heterocycles by Ni/Photoredox Dual Catalysis by Lacker, Caitlin R., DeLano, Travis J., Chen, Emily P., Kong, Jongrock, Belyk, Kevin M., Piou, Tiffany, Reisman, Sarah E.

“…An asymmetric cross-coupling of α-N-heterocyclic trifluoroborates with aryl bromides using Ni/photoredox dual catalysis has been developed. This…”
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Enantio- and Diastereoselective Total Synthesis of Belzutifan Enabled by Rh-Catalyzed Hydrogenation by Le, Diane N., Johnson, Heather C., Lam, Yu-hong, Sun, Chunrui, Cheng, Lili, Belyk, Kevin M.

“…Herein, we report a nine-step synthesis of belzutifan enabled by a novel Rh-catalyzed asymmetric hydrogenation to install the contiguous fluorinated…”
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Enantioselective Rh(I)-Catalyzed Addition of Arylboronic Acids to Cyclic Ketimines by Kong, Jongrock, McLaughlin, Mark, Belyk, Kevin, Mondschein, Ryan

“…A method for the enantioselective synthesis of chiral α-tertiary amines via Rh-catalyzed 1,2-addition of arylboronic acids to cyclic ketimines is described…”
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Rhodium-Catalyzed Enantioselective Addition of Boronic Acids to N-Benzylnicotinate Salts by Christian, Nadeau, Aly, Sara, Belyk, Kevin

“…The highly enantioselective catalytic asymmetric addition of aryl and alkenylboronic acids to N-benzylnicotinate salt 1 is described. The dihydropyridine 2…”
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Late‐Stage Modification of Oligopeptides by Nickel‐Catalyzed Stereoselective Radical Addition to Dehydroalanine by Qi, Xiaoxu, Jambu, Subramanian, Ji, Yining, Belyk, Kevin M., Panigrahi, Nihar R., Arora, Paramjit S., Strotman, Neil A., Diao, Tianning

“…Radical addition to dehydroalanine (Dha) represents an appealing, modular strategy to access non‐canonical peptide analogues for drug discovery. Prior studies…”
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Enantioselective Synthesis of Hemiaminals via Pd-Catalyzed C–N Coupling with Chiral Bisphosphine Mono-oxides by Li, Hongming, Belyk, Kevin M, Yin, Jingjun, Chen, Qinghao, Hyde, Alan, Ji, Yining, Oliver, Steven, Tudge, Matthew T, Campeau, Louis-Charles, Campos, Kevin R

“…A novel approach to hemiaminal synthesis via palladium-catalyzed C–N coupling with chiral bisphosphine mono-oxides is described. This efficient new method…”
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Application of Machine Learning and Reaction Optimization for the Iterative Improvement of Enantioselectivity of Cinchona-Derived Phase Transfer Catalysts by Lexa, Katrina W, Belyk, Kevin M, Henle, Jeremy, Xiang, Bangping, Sheridan, Robert P, Denmark, Scott E, Ruck, Rebecca T, Sherer, Edward C

“…Molecular design benefits from a strong partnership between chemical intuition and machine learning. Given the proliferation of machine learning in the small…”
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Enantioselective Synthesis of 4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) via Enzymatic Desymmetrization by McLaughlin, Mark, Kong, Jongrock, Belyk, Kevin M, Chen, Billy, Gibson, Andrew W, Keen, Stephen P, Lieberman, David R, Milczek, Erika M, Moore, Jeffrey C, Murray, David, Peng, Feng, Qi, Ji, Reamer, Robert A, Song, Zhiguo J, Tan, Lushi, Wang, Lin, Williams, Michael J

“…An enantioselective synthesis of the potent anti-HIV nucleoside EFdA is presented. Key features of stereocontrol include construction of the fully substituted…”
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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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A Robust Kilo-Scale Synthesis of Doravirine by Campeau, Louis-Charles, Chen, Qinghao, Gauvreau, Danny, Girardin, Mélina, Belyk, Kevin, Maligres, Peter, Zhou, Guoyue, Gu, Chaozhan, Zhang, Wei, Tan, Lushi, O’Shea, Paul D

“…Doravirine is non-nucleoside reverse transcriptase inhibitor (NNRTI) currently in phase III clinical trials for the treatment of HIV infection. Herein we…”
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A rational pre-catalyst design for bis-phosphine mono-oxide palladium catalyzed reactions by Ji, Yining, Li, Hongming, Hyde, Alan M, Chen, Qinghao, Belyk, Kevin M, Lexa, Katrina W, Yin, Jingjun, Sherer, Edward C, Williamson, R Thomas, Brunskill, Andrew, Ren, Sumei, Campeau, Louis-Charles, Davies, Ian W, Ruck, Rebecca T

“…Significant catalyst loading reduction and increased reaction robustness have been achieved for a Pd-catalyzed asymmetric intramolecular C-N coupling through…”
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Late‐Stage Modification of Oligopeptides by Nickel‐Catalyzed Stereoselective Radical Addition to Dehydroalanine by Qi, Xiaoxu, Jambu, Subramanian, Ji, Yining, Belyk, Kevin M., Panigrahi, Nihar R., Arora, Paramjit S., Strotman, Neil A., Diao, Tianning

“…Radical addition to dehydroalanine (Dha) represents an appealing, modular strategy to access non‐canonical peptide analogues for drug discovery. Prior studies…”
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Synthesis of Vaniprevir (MK-7009): Lactamization To Prepare a 22-Membered Macrocycle by Song, Zhiguo J, Tellers, David M, Journet, Michel, Kuethe, Jeffrey T, Lieberman, David, Humphrey, Guy, Zhang, Fei, Peng, Zhihui, Waters, Marjorie S, Zewge, Daniel, Nolting, Andrew, Zhao, Dalian, Reamer, Robert A, Dormer, Peter G, Belyk, Kevin M, Davies, Ian W, Devine, Paul N, Tschaen, David M

“…Development of a practical synthesis of MK-7009, a 22-membered macrocycle, is described. A variety of ring-closing strategies were evaluated, including…”
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Synthesis of α-Hydroxyacetophenones by McLaughlin, Mark, Belyk, Kevin M, Qian, Gang, Reamer, Robert A, Chen, Cheng-yi

“…A general method for the preparation of α-hydroxyacetophenones is presented. Functionalized arylmagnesium species are transmetalated to the corresponding…”
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Enantioselective Synthesis of (1R,2S)-1-Amino-2-vinylcyclopropanecarboxylic Acid Ethyl Ester (Vinyl-ACCA-OEt) by Asymmetric Phase-Transfer Catalyzed Cyclopropanation of (E)-N-Phenylmethyleneglycine Ethyl Ester by Belyk, Kevin M, Xiang, Bangping, Bulger, Paul G, Leonard, William R, Balsells, Jaume, Yin, Jingjun, Chen, Cheng-yi

“…A concise asymmetric synthesis of (1R,2S)-1-amino-2-vinylcyclopropanecarboxylic acid ethyl ester, a key intermediate in the preparation of many hepatitis C…”
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Practical Asymmetric Synthesis of a Chiral Piperazinone Derivative by McLaughlin, Mark, Belyk, Kevin, Chen, Cheng-yi, Linghu, Xin, Pan, Jun, Qian, Gang, Reamer, Robert A, Xu, Yingju

“…A practical asymmetric route to a chiral piperazinone derivative, a fragment of MK-3207, is reported. The amine-bearing benzylic stereocenter is introduced via…”
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Development of a Second-Generation, Highly Efficient Manufacturing Route for the HIV Integrase Inhibitor Raltegravir Potassium by Humphrey, Guy R, Pye, Philip J, Zhong, Yong-Li, Angelaud, Remy, Askin, David, Belyk, Kevin M, Maligres, Peter E, Mancheno, Danny E, Miller, Ross A, Reamer, Robert A, Weissman, Steven A

“…A manufacturing route for the synthesis of raltegravir potassium 1 was developed via a thermal rearrangement of amidoxime DMAD adducts 6 to construct the key,…”
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Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain by Chobanian, Harry R, Guo, Yan, Liu, Ping, Chioda, Marc D, Fung, Selena, Lanza, Thomas J, Chang, Linda, Bakshi, Raman K, Dellureficio, James P, Hong, Qingmei, McLaughlin, Mark, Belyk, Kevin M, Krska, Shane W, Makarewicz, Amanda K, Martel, Elliot J, Leone, Joseph F, Frey, Lisa, Karanam, Bindhu, Madeira, Maria, Alvaro, Raul, Shuman, Joyce, Salituro, Gino, Terebetski, Jenna L, Jochnowitz, Nina, Mistry, Shruti, McGowan, Erin, Hajdu, Richard, Rosenbach, Mark, Abbadie, Catherine, Alexander, Jessica P, Shiao, Lin-Lin, Sullivan, Kathleen M, Nargund, Ravi P, Wyvratt, Matthew J, Lin, Linus S, DeVita, Robert J

“…We report herein the identification of MK-4409, a potent and selective fatty acid amide hydrolase (FAAH) inhibitor. Starting from a high throughput screening…”
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Synthesis of the Antifungal β-1,3-Glucan Synthase Inhibitor CANCIDAS (Caspofungin Acetate) from Pneumocandin B0 by Leonard, William R, Belyk, Kevin M, Conlon, David A, Bender, Dean R, DiMichele, Lisa M, Liu, Ji, Hughes, David L

“…A novel three-step synthesis of the highly functionalized antifungal agent CANCIDAS (caspofungin acetate, 2) is described, starting from the natural product…”
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