G
Gregory Hughes
Researcher at Merck & Co.
Publications - 16
Citations - 1845
Gregory Hughes is an academic researcher from Merck & Co.. The author has contributed to research in topics: Imine & Tertiary amine. The author has an hindex of 7, co-authored 16 publications receiving 1531 citations. Previous affiliations of Gregory Hughes include Codexis & Genentech.
Papers
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Journal ArticleDOI
Biocatalytic Asymmetric Synthesis of Chiral Amines from Ketones Applied to Sitagliptin Manufacture
Christopher Savile,Jacob M. Janey,Emily Mundorff,Jeffrey C. Moore,Sarena Tam,William R. Jarvis,Jeffrey Colbeck,Anke Krebber,Fred J. Fleitz,Jos Brands,Paul N. Devine,Gjalt W. Huisman,Gregory Hughes +12 more
TL;DR: An efficient biocatalytic process to replace a recently implemented rhodium-catalyzed asymmetric enamine hydrogenation for the large-scale manufacture of the antidiabetic compound sitagliptin is reported, underscoring the maturation of bioc atalysis to enable efficient, economical, and environmentally benign processes for the manufacture of pharmaceuticals.
Journal ArticleDOI
Design of an in vitro biocatalytic cascade for the manufacture of islatravir
Mark A. Huffman,Anna Fryszkowska,Oscar Alvizo,Margie Borra-Garske,Kevin R. Campos,Canada Keith A,Paul N. Devine,Da Duan,Jacob Forstater,Shane T. Grosser,Holst M. Halsey,Gregory Hughes,Junyong Jo,Leo A. Joyce,Joshua N. Kolev,Jack Liang,Kevin M. Maloney,Benjamin F. Mann,Nicholas M. Marshall,Mark McLaughlin,Jeffrey C. Moore,Grant S. Murphy,Christopher C. Nawrat,Jovana Nazor,Scott J. Novick,Niki R. Patel,Agustina Rodriguez-Granillo,Sandra A. Robaire,Edward C. Sherer,Matthew D. Truppo,Aaron M. Whittaker,Deeptak Verma,Li Xiao,Yingju Xu,Hao Yang +34 more
TL;DR: An in vitro biocatalytic cascade synthesis of the investigational HIV treatment islatravir is reported, requiring fewer than half the number of steps of the previously reported routes.
Journal ArticleDOI
Sustainable Practices in Medicinal Chemistry: Current State and Future Directions
Marian C. Bryan,Barry Dillon,Lawrence G. Hamann,Gregory Hughes,Michael E. Kopach,Emily A. Peterson,Pourashraf Mehrnaz,Izzat T. Raheem,Paul G. Richardson,Daniel Tyler Richter,Helen F. Sneddon +10 more
TL;DR: The medicinal chemistry subgroup of the American Chemical Society's Green Chemistry Institute Pharmaceutical Roundtable (ACS GCI PR) offers a perspective on the current state of environmentally sustainable practices in medicinal chemistry with the aim of sharing best practices more widely and highlighting some potential future developments.
Journal ArticleDOI
Ligand-Dependent Site-Selective Suzuki Cross-Coupling of 3,5-Dichloropyridazines
Xing Dai,Yonggang Chen,Stephanie Garrell,Hong Liu,Li-Kang Zhang,Anandan Palani,Gregory Hughes,Ravi P. Nargund +7 more
TL;DR: General methods for the highly site-selective Suzuki monocoupling of 3,5-dichloropyridazines have been discovered, enabling the rapid construction of diverse arrays of diarylpyradazines in a modular fashion.
Patent
Engineered imine reductases and methods for the reductive amination of ketone and amine compounds
Haibin Chen,Steven J. Collier,Jovana Nazor,Joly Sukumaran,Derek Smith,Jeffrey C. Moore,Gregory Hughes,Jacob Janey,Gjalt W. Huisman,Scott J. Novick,Nicholas J. Agard,Oscar Alvizo,Gregory A. Cope,Wan Lin Yeo,Stefanie Ng Minor +14 more
TL;DR: The present disclosure provides engineered polypeptides having imine reductase activity, polynucleotides encoding the engineered imine reduction enzymes, host cells capable of expressing the engineered reductases, and methods of using these engineered PU with a range of ketone and amine substrate compounds to prepare secondary and tertiary amine product compounds as mentioned in this paper.