80696-29-3Relevant articles and documents
Enantioselective Synthesis of Chiral Vicinal Amino Alcohols Using Amine Dehydrogenases
Chen, Fei-Fei,Cosgrove, Sebastian C.,Birmingham, William R.,Mangas-Sanchez, Juan,Citoler, Joan,Thompson, Matthew P.,Zheng, Gao-Wei,Xu, Jian-He,Turner, Nicholas J.
, p. 11813 - 11818 (2019)
Chiral vicinal amino alcohols are an important motif found in many biologically active molecules. In this study, biocatalytic reductive amination of α-hydroxy ketones with ammonia was investigated using engineered amine dehydrogenases (AmDHs) derived from the leucine amino acid dehydrogenase (AADH) from Lysinibacillus fusiformis. The AmDHs thus identified enabled the synthesis of (S)-configured vicinal amino alcohols from the corresponding α-hydroxy ketones in up to 99% conversions and >99% ee. One of the AmDH variants was used to prepare a key intermediate for the antituberculosis pharmaceutical ethambutol.
COMPOUNDS AND METHOD OF USE
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Paragraph 1426, (2019/09/06)
This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.
Discovery of narlaprevir (SCH 900518): A potent, second generation HCV NS3 serine protease inhibitor
Arasappan, Ashok,Bennett, Frank,Bogen, Stephane L.,Venkatraman, Srikanth,Blackman, Melissa,Chen, Kevin X.,Hendrata, Siska,Huang, Yuhua,Huelgas, Regina M.,Nair, Latha,Padilla, Angela I.,Pan, Weidong,Pike, Russell,Pinto, Patrick,Ruan, Sumei,Sannigrahi, Mousumi,Velazquez, Francisco,Vibulbhan, Bancha,Wu, Wanli,Yang, Weiying,Saksena, Anil K.,Girijavallabhan, Viyyoor,Shih, Neng-Yang,Kong, Jianshe,Meng, Tao,Jin, Yan,Wong, Jesse,McNamkra, Paul,Prongay, Andrew,Madison, Vincent,Piwinski, John J.,Cheng, Kuo-Chi,Morrison, Richard,Malcolm, Bruce,Tong, Xiao,Ralston, Robert,Njoroge, F. George
scheme or table, p. 64 - 69 (2010/12/29)
Boceprevir (SCH 503034), 1, a novel HCV NS3 serine protease inhibitor discovered in our laboratories, is currently undergoing phase III clinical trials. Detailed investigations toward a second generation protease inhibitor culminated in the discovery of narlaprevir (SCH 900518), 37, with improved potency (～10-fold over 1), pharmacokinetic profile and physicochemical characteristics, currently in phase II human trials. Exploration of synthetic sequence for preparation of 37 resulted in a route that required no silica gel purification for the entire synthesis.
