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138 results on '"Rivera, Nelo"'

1. A kinase-cGAS cascade to synthesize a therapeutic STING activator

Author

McIntosh, John A., Liu, Zhijian, Andresen, Brian M., Marzijarani, Nastaran Salehi, Moore, Jeffrey C., Marshall, Nicholas M., Borra-Garske, Margie, Obligacion, Jennifer V., Fier, Patrick S., Peng, Feng, Forstater, Jacob H., Winston, Matthew S., An, Chihui, Chang, Wonsuk, Lim, Jongwon, Huffman, Mark A., Miller, Steven P., Tsay, Fuh-Rong, Altman, Michael D., Lesburg, Charles A., Steinhuebel, Dietrich, Trotter, B. Wesley, Cumming, Jared N., Northrup, Alan, Bu, Xiaodong, Mann, Benjamin F., Biba, Mirlinda, Hiraga, Kaori, Murphy, Grant S., Kolev, Joshua N., Makarewicz, Amanda, Pan, Weilan, Farasat, Iman, Bade, Rachel S., Stone, Kevin, Duan, Da, Alvizo, Oscar, Adpressa, Donovan, Guetschow, Erik, Hoyt, Erik, Regalado, Erik L., Castro, Steve, Rivera, Nelo, Smith, Joseph P., Wang, Fengqiang, Crespo, Alejandro, Verma, Deeptak, Axnanda, Stephanus, Dance, Zachary E. X., Devine, Paul N., Tschaen, David, Canada, Keith A., Bulger, Paul G., Sherry, Benjamin D., Truppo, Matthew D., Ruck, Rebecca T., Campeau, Louis-Charles, Bennett, David Jonathan, Humphrey, Guy R., Campos, Kevin R., and Maddess, Matthew L.

Published
2022
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3. Use of a Dynamic Flow Platform To Translate a Batch Immobilized Transaminase Process to a Packed Bed Reactor for the Synthesis of an Intermediate of Nemtabrutinib.

Author

Di Maso, Michael J., Kuethe, Jeffrey T., Narsimhan, Karthik, Burris, Matthew, Chung, Cheol K., DiBenedetto, Michael, Forstater, Jacob H., Grosser, Shane T., Kuhl, Nadine, Lévesque, François, Maguire, Anne, Maloney, Kevin M., McMullen, Jonathan P., Prier, Christopher K., Qi, Ji, Rivera, Nelo R., Wang, Zhixun, Wyvratt, Brian M., and Zewge, Daniel

Published
2024
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5. Amination of a Green Solvent via Immobilized Biocatalysis for the Synthesis of Nemtabrutinib

Author

Prier, Christopher K., primary, Camacho Soto, Karla, additional, Forstater, Jacob H., additional, Kuhl, Nadine, additional, Kuethe, Jeffrey T., additional, Cheung-Lee, Wai Ling, additional, Di Maso, Michael J., additional, Eberle, Claire M., additional, Grosser, Shane T., additional, Ho, Hsing-I, additional, Hoyt, Erik, additional, Maguire, Anne, additional, Maloney, Kevin M., additional, Makarewicz, Amanda, additional, McMullen, Jonathan P., additional, Moore, Jeffrey C., additional, Murphy, Grant S., additional, Narsimhan, Karthik, additional, Pan, Weilan, additional, Rivera, Nelo R., additional, Saha-Shah, Anumita, additional, Thaisrivongs, David A., additional, Verma, Deeptak, additional, Wyatt, Adeya, additional, and Zewge, Daniel, additional

Published
2023
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6. Gefapixant Citrate (MK-7264) Sulfonamide Step Speciation Study: Investigation into Precipitation–Dissolution Events during Addition of Chlorosulfonic Acid

Author

Rivera, Nelo R., primary, Cohen, Ryan D., additional, Zhang, Si-Wei, additional, Dance, Zachary E. X., additional, Halsey, Holst M., additional, Song, Siqing, additional, Bu, Xiaodong, additional, Reibarkh, Mikhail, additional, Ren, Hong, additional, Lee, Alfred Y., additional, Chang, Darryl, additional, and Lohani, Sachin, additional

Published
2023
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7. Utilizing biocatalysis and a sulfolane-mediated reductive acetal opening to access nemtabrutinib from cyrene

Author

Kuhl, Nadine, primary, Turnbull, Ben W. H., additional, Ji, Yining, additional, Larson, Reed T., additional, Shevlin, Michael, additional, Prier, Christopher K., additional, Chung, Cheol K., additional, Desmond, Richard, additional, Guetschow, Erik, additional, He, Cyndi Qixin, additional, Itoh, Tetsuji, additional, Kuethe, Jeffrey T., additional, Newman, Justin A., additional, Reibarkh, Mikhail, additional, Rivera, Nelo R., additional, Shang, Gao, additional, Wang, Zhixun, additional, Zewge, Daniel, additional, and Thaisrivongs, David A., additional

Published
2023
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8. Utilizing Biocatalysis and an Unprecedented Sulfolane-mediated Reductive Acetal Opening to Access Nemtabrutinib from Cyrene

Author

Kuhl, Nadine, primary, Turnbull, Ben W. H., additional, Ji, Yining, additional, Larson, Reed T., additional, Shevlin, Michael, additional, Prier, Christopher K., additional, Chung, Cheol K., additional, Desmond, Richard, additional, Guetschow, Erik, additional, He, Cyndi Qixin, additional, Itoh, Tetsuji, additional, Kuethe, Jeffrey T., additional, Newman, Justin A., additional, Reibarkh, Mikhail, additional, Rivera, Nelo R., additional, Shang, Gao, additional, Wang, Zhixun, additional, Zewge, Daniel, additional, and Thaisrivongs, David A., additional

Published
2022
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9. Iron-catalysed tritiation of pharmaceuticals

Author

Pony Yu, Renyuan, Hesk, David, Rivera, Nelo, Pelczer, István, and Chirik, Paul J.

Subjects
Catalysis -- Methods, Iron catalysts -- Mechanical properties -- Structure, Drugs -- Analysis, Tritium -- Usage, Environmental issues, Science and technology, Zoology and wildlife conservation
Abstract

An iron-catalysed method for the direct .sup.3H labelling of pharmaceuticals by hydrogen isotope exchange using tritium gas is reported; the site selectivity of the iron catalyst is orthogonal to currently used iridium catalysts and allows isotopic labelling of complementary positions in drug molecules. Iron-catalysed tritium labelling Radiolabelled compounds, usually containing .sup.14C or .sup.3H, are a powerful tool in pharmacokinetics and diagnostics. In this manuscript, the authors describe a new iron-catalysed method for the direct .sup.3H labelling of pharmaceuticals by hydrogen isotope exchange using tritium gas as the source of the radioisotope. The site selectivity of the iron catalyst is orthogonal to currently used iridium catalysts and allows isotopic labeling of complementary positions in drug molecules, providing a new diagnostic tool in drug development. A thorough understanding of the pharmacokinetic and pharmacodynamic properties of a drug in animal models is a critical component of drug discovery and development.sup.1,2,3,4,5,6. Such studies are performed in vivo and in vitro at various stages of the development process--ranging from preclinical absorption, distribution, metabolism and excretion (ADME) studies to late-stage human clinical trials--to elucidate a drug molecule's metabolic profile and to assess its toxicity.sup.2. Radiolabelled compounds, typically those that contain .sup.14C or .sup.3H isotopes, are one of the most powerful and widely deployed diagnostics for these studies.sup.4,5. The introduction of radiolabels using synthetic chemistry enables the direct tracing of the drug molecule without substantially altering its structure or function. The ubiquity of C-H bonds in drugs and the relative ease and low cost associated with tritium (.sup.3H) make it an ideal radioisotope with which to conduct ADME studies early in the drug development process.sup.2,4,6. Here we describe an iron-catalysed method for the direct .sup.3H labelling of pharmaceuticals by hydrogen isotope exchange, using tritium gas as the source of the radioisotope. The site selectivity of the iron catalyst is orthogonal to currently used iridium catalysts and allows isotopic labelling of complementary positions in drug molecules, providing a new diagnostic tool in drug development., Author(s): Renyuan Pony Yu [sup.1] , David Hesk [sup.2] , Nelo Rivera [sup.2] , István Pelczer [sup.1] , Paul J. Chirik [sup.1] Author Affiliations: (1) Department of Chemistry, Princeton University, [...]

Published
2016
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10. Iron-catalysed tritiation of pharmaceuticals

Author

Yu, Renyuan Pony, Hesk, David, Rivera, Nelo, Pelczer, Istvan, and Chirik, Paul J.

Subjects
Drug discovery -- Analysis, Deuterium -- Research -- Influence, Environmental issues, Science and technology, Zoology and wildlife conservation
Abstract

A thorough understanding of the pharmacokinetic and pharmacodynamic properties of a drug in animal models is a critical component of drug discovery and development (1-6). Such studies are performed in vivo and in vitro at various stages of the development process--ranging from preclinical absorption, distribution, metabolism and excretion (ADME) studies to late-stage human clinical trials--to elucidate a drug molecule's metabolic profile and to assess its toxicity (2). Radiolabelled compounds, typically those that contain [sup.14]C or ³H isotopes, are one of the most powerful and widely deployed diagnostics for these studies (4,5). The introduction of radiolabels using synthetic chemistry enables the direct tracing of the drug molecule without substantially altering its structure or function. The ubiquity of C-H bonds in drugs and the relative ease and low cost associated with tritium (³H) make it an ideal radioisotope with which to conduct ADME studies early in the drug development process (2,4,6). Here we describe an iron-catalysed method for the direct ³H labelling of pharmaceuticals by hydrogen isotope exchange, using tritium gas as the source of the radioisotope. The site selectivity of the iron catalyst is orthogonal to currently used iridium catalysts and allows isotopic labelling of complementary positions in drug molecules, providing a new diagnostic tool in drug development., Deuterium- and tritium-labelled compounds find widespread application in the pharmaceutical industry because of their ability to alter metabolism (7,8), to exploit kinetic isotope effects (9) and most commonly to perform [...]

Published
2016

11. Methods for the synthesis of 5,6,7,8-tetrahydro-1,8-naphthyridine fragments for (alpha)v(beta)3 integrin antagonists

Author

Hartner, Frederick W., Yi Hsiao, Kan K. Eng, Rivera, Nelo R., Palucki, Michael, Tschaen, Dave, Volante, R.P., Tan, Lushi, Yasuda, Nobuyoshi, Hughes, David L., Weissman, Steven, Zewge, Daniel, and King, Tony

Subjects
Osteoporosis -- Care and treatment, Osteoporosis -- Research, Chemical synthesis -- Observations, Biological sciences, Chemistry
Abstract

The preparation of 3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propan-1-amine and 3-[7R)-7-methyl-5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl]propan-1-amine, key intermediates in the synthesis of (alpha)v(beta)3 antagonists is described.

Published
2004

13. Correction to “Highly Efficient Asymmetric Synthesis of Sitagliptin”

Author

Hansen, Karl B., primary, Hsiao, Yi, additional, Xu, Feng, additional, Rivera, Nelo, additional, Clausen, Andrew, additional, Kubryk, Michele, additional, Krska, Shane, additional, Rosner, Thorsten, additional, Simmons, Bryon, additional, Balsells, Jaume, additional, Ikemoto, Nori, additional, Sun, Yongkui, additional, Spindler, Felix, additional, Malan, Christophe, additional, Grabowski, Edward J. J., additional, and Armstrong, Joseph D., additional

Published
2020
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21. Highly efficient asymmetric synthesis of sitagliptin

Author

Hansen, Karl B., Yi Hsiao, Feng Xu, Rivera, Nelo, Clausen, Andrew, Kubryk, Michele, Krska, Shane, Rosner, Thorsten, Balsells, Jaume, Simmons, Bryon, Ikemoto, Nori, Yongkui Sun, Spindler, Felix, Malan, Christophe, Grabowski, Edward J.J., and Armstrong, Joseph D., III

Subjects
Green chemistry -- Research, Hydrogenation -- Analysis, Sitagliptin -- Structure, Sitagliptin -- Chemical properties, Sitagliptin -- Environmental aspects, Type 2 diabetes -- Drug therapy, Chemistry
Abstract

A highly efficient synthesis of sitagliptin, a potent and selective DPP-4 inhibitor for the treatment of type 2 diabetes mellitus (T2DM), is developed. The green synthesis has reduced the total waste generated per kilogram of sitagliptin produced in comparison with the first-generation route and has eliminated aqueous waste streams.

Published
2009

22. An efficient synthesis of an alpha(sub v)beta(sub 3) antagonist

Author

Yasuda, Nobuyoshi, Yi Hsiao, Jensen, Mark S., Rivera, Nelo R., Chunhua Yang, Wells, Kenneth M., Yau, James, Palucki, Michael, Tan, Lushi, Dormer, Peter G., Volante, Ralph P., Hughes, David L., and Reider, Paul J.

Subjects
Ring formation (Chemistry) -- Observations, Alanine -- Research, Osteoporosis -- Research, Biological sciences, Chemistry
Abstract

A practical preparation of an alpha(sub v)beta(sub 3) antagonist is reported. The antagonist consists of three key components that were prepared in various methods, due to which a highly convergent process for the drug candidate was defined.

Published
2004

24. Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys

Author

Hoyt, Scott B., primary, Park, Min K., additional, London, Clare, additional, Xiong, Yusheng, additional, Tata, Jim, additional, Bennett, D. Jonathan, additional, Cooke, Andrew, additional, Cai, Jiaqiang, additional, Carswell, Emma, additional, Robinson, John, additional, MacLean, John, additional, Brown, Lindsay, additional, Belshaw, Simone, additional, Clarkson, Thomas R., additional, Liu, Kun, additional, Liang, Gui-Bai, additional, Struthers, Mary, additional, Cully, Doris, additional, Wisniewski, Tom, additional, Ren, Ning, additional, Bopp, Charlene, additional, Sok, Andrea, additional, Cai, Tian-Quan, additional, Stribling, Sloan, additional, Pai, Lee-Yuh, additional, Ma, Xiuying, additional, Metzger, Joe, additional, Verras, Andreas, additional, McMasters, Daniel, additional, Chen, Qing, additional, Tung, Elaine, additional, Tang, Wei, additional, Salituro, Gino, additional, Buist, Nicole, additional, Kuethe, Jeff, additional, Rivera, Nelo, additional, Clemas, Joe, additional, Zhou, Gaochao, additional, Gibson, Jack, additional, Maxwell, Carrie Ann, additional, Lassman, Mike, additional, McLaughlin, Theresa, additional, Castro-Perez, Jose, additional, Szeto, Daphne, additional, Forrest, Gail, additional, Hajdu, Richard, additional, Rosenbach, Mark, additional, and Ali, Amjad, additional

Published
2015
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25. Highly efficient synthesis of Beta-amino acid derivatives via asymmetric hydrogenation of unprotected enamines

Author

Yi Hsiao, Rivera, Nelo R., Rosner, Thorsten, Krska, Shane W., Njolito, Eugenia, Wang, Fang, Sun, Yongkui, Armstrong, Joseph D., Grabowski, Edward J. J., Tillyer, Richard D., Spindler, Felix, and Malan Christophe

Subjects
Esters -- Chemical properties, Amines -- Chemical properties, Hydrogenation -- Analysis, Chemistry
Abstract

The first general method of high yielding, highly enantioselective hydrogenations of unprotected Beta-enamine esters 1 and amides 3 are reported for which legends under mild hydrogenation conditions are used. The method gives high enantioselectivity, high reactivity and wide applicability, which require no protecting groups.

Published
2004

26. Highly diastereoselective heterogeneously catalyzed hydrogenation of enamines for the synthesis of chiral beta-amino acid derivatives

Author

Ikemoto, Norihiro, Rivera, Nelo R., Armstrong, Joseph D., III, Tellers, David M., Njolito, Eugenia, Yongkui Sun, Dreher, Spencer D., Yi Hsiao, Mathre, David J., Liu Jinchu, McWilliams, J. Christopher, Grabowski, Edward J.J., Huang Angie, Williams, J. Michael, and Tillyer, Richard D.

Subjects
Chemical synthesis -- Research, Diastereomers -- Research, Hydrogenation -- Research, Amides -- Research, Chemistry
Abstract

A new set of conditions was identified for the preparation of beta-aminoesters and amides that is heterogeneous catalysis with unprecedented diastereoselectivities and good substrate generality. This approach offers an alternative synthetic strategy to asymmetric hydrogenation methods.

Published
2004

39. Stereoselective synthesis of an anti-HIV drug candidate

Author

Conlon, David A., primary, Jensen, Mark S., additional, Palucki, Michael, additional, Yasuda, Nobuyoshi, additional, Um, Joann M., additional, Yang, Chunhua, additional, Hartner, Frederick W., additional, Tsay, Fuh-Rong, additional, Hsiao, Yi, additional, Pye, Philip, additional, Rivera, Nelo R., additional, and Hughes, David L., additional

Published
2005
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41. Methods for the Synthesis of 5,6,7,8-Tetrahydro-1,8-naphthyridine Fragments for αVβ3 Integrin Antagonists

Author

Hartner, Frederick W., primary, Hsiao, Yi, additional, Eng, Kan K., additional, Rivera, Nelo R., additional, Palucki, Michael, additional, Tan, Lushi, additional, Yasuda, Nobuyoshi, additional, Hughes, David L., additional, Weissman, Steven, additional, Zewge, Daniel, additional, King, Tony, additional, Tschaen, Dave, additional, and Volante, R. P., additional

Published
2004
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42. Highly Efficient Synthesis of β-Amino Acid Derivatives via Asymmetric Hydrogenation of Unprotected Enamines

Author

Hsiao, Yi, primary, Rivera, Nelo R., additional, Rosner, Thorsten, additional, Krska, Shane W., additional, Njolito, Eugenia, additional, Wang, Fang, additional, Sun, Yongkui, additional, Armstrong, Joseph D., additional, Grabowski, Edward J. J., additional, Tillyer, Richard D., additional, Spindler, Felix, additional, and Malan, Christophe, additional

Published
2004
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44. An Efficient Synthesis of an αvβ3 Antagonist

Author

Yasuda, Nobuyoshi, primary, Hsiao, Yi, additional, Jensen, Mark S., additional, Rivera, Nelo R., additional, Yang, Chunhua, additional, Wells, Kenneth M., additional, Yau, James, additional, Palucki, Michael, additional, Tan, Lushi, additional, Dormer, Peter G., additional, Volante, Ralph P., additional, Hughes, David L., additional, and Reider, Paul J., additional

Published
2004
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