16149-05-6Relevant academic research and scientific papers
Hydrogen bond directed aerobic oxidation of amines via photoredox catalysis
Wang, Hongyu,Man, Yunquan,Wang, Kaiye,Wan, Xiuyan,Tong, Lili,Li, Na,Tang, Bo
, p. 10989 - 10992 (2018/10/08)
An application of H-bonding interactions for directing the α-C-H oxidation of amines to amides and amino-ketones catalyzed by an organic photocatalyst is reported. The high efficiency of this method is demonstrated by the aerobic oxidation of pyrrolidines, diarylamines and benzylamines bearing urea groups with high yields and a wide substrate scope.
COMPOUNDS AND METHODS FOR TREATING RESPIRATORY DISEASES
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Page/Page column 26, (2011/11/12)
Described herein are compounds and compositions, and methods for using the compounds and compositions, for treating respiratory diseases and illness, such as severe acute respiratory syndrome (SARS).
Structure-based design, synthesis, and biological evaluation of a series of novel and reversible inhibitors for the severe acute respiratory syndrome - Coronavirus papain-like protease
Ghosh, Arun K.,Takayama, Jun,Aubin, Yoann,Ratia, Kiira,Chaudhuri, Rima,Baez, Yahira,Sleeman, Katrina,Coughlin, Melissa,Nichols, Daniel B.,Mulhearn, Debbie C.,Prabhakar, Bellur S.,Baker, Susan C.,Johnson, Michael E.,Mesecar, Andrew D.
experimental part, p. 5228 - 5240 (2010/03/04)
We describe here the design, synthesis, molecular modeling, and biological evaluation of a series of small molecule, nonpeptide inhibitors of SARS-CoV PLpro. Our initial lead compound was identified via high-throughput screening of a diverse chemical library. We subsequently carried out structure - activity relationship studies and optimized the lead structure to potent inhibitors that have shown antiviral activity against SARS-CoV infected Vero E6 cells. Upon the basis of the X-ray crystal structure of inhibitor 24-bound to SARS-CoV PLpro, a drug design template was created. Our structure-based modification led to the design of a more potent inhibitor, 2 (enzyme IC50 = 0.46 μM; antiviral EC50 = 6 μM). Interestingly, its methylamine derivative, 49, displayed good enzyme inhibitory potency (IC50 = 1.3 μM) and the most potent SARS antiviral activity (EC50 = 5.2 μM) in the series. We have carried out computational docking studies and generated a predictive 3D-QSAR model for SARS-CoV PLpro inhibitors.
Rapid, one-pot synthesis of α,α-disubstituted primary amines by the addition of Grignard reagents to nitriles under microwave heating conditions
Gregg, Brian T.,Golden, Kathryn C.,Quinn, John F.,Wang, Hong-Jun,Zhang, Wei,Wang, Ruifang,Wekesa, Francis,Tymoshenko, Dmytro O.
experimental part, p. 3978 - 3981 (2009/10/04)
A series of α,α-disubstituted amines have been prepared in a simple and efficient one-pot procedure by the addition of Grignard reagents to a series of aliphatic, aromatic, and heteroaromatic nitriles. Key to this reported procedure is the unprecedented addition of the Grignard reagent to the nitrile under heating by microwave irradiation which both significantly improves reaction yields and reduces reaction times. In general, the Grignard addition reaction is complete within 5-10 min at 100 °C followed by rapid reduction with sodium borohydride to give the target amines.
