- Synthesis of α-Amidoketones through the Cascade Reaction of Carboxylic Acids with Vinyl Azides under Catalyst-Free Conditions
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An efficient synthesis of α-amidoketone derivatives through the cascade reactions of carboxylic acids with vinyl azides is presented. Compared with literature protocols, notable features of this new method include catalyst-free conditions, broad substrate scope, good tolerance of a wide range of functional groups, and high efficiency. In addition, the synthetic potential of this method as a tool for late-stage modification was convincingly manifested by its application in the structural elaborations of a number of carboxylic acid drug molecules.
- Gao, Cai,Zhou, Qianting,Yang, Li,Zhang, Xinying,Fan, Xuesen
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p. 13710 - 13720
(2020/11/13)
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- Discovery of novel VX-809 hybrid derivatives as F508del-CFTR correctors by molecular modeling, chemical synthesis and biological assays
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Cystic fibrosis (CF) is the autosomal recessive disorder most recurrent in Caucasian populations. It is caused by different mutations in the cystic fibrosis transmembrane regulator protein (CFTR) gene, with F508del being the most common. During the last y
- Parodi, Alice,Righetti, Giada,Pesce, Emanuela,Salis, Annalisa,Tasso, Bruno,Urbinati, Chiara,Tomati, Valeria,Damonte, Gianluca,Rusnati, Marco,Pedemonte, Nicoletta,Cichero, Elena,Millo, Enrico
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- Structure-Activity Relationships of New Natural Product-Based Diaryloxazoles with Selective Activity against Androgen Receptor-Positive Breast Cancer Cells
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Targeted therapies for ER+/PR+ and HER2-amplified breast cancers have improved patient survival, but there are no therapies for triple negative breast cancers (TNBC) that lack expression of estrogen and progesterone receptors (ER/PR), or amplification or
- Robles, Andrew J.,McCowen, Shelby,Cai, Shengxin,Glassman, Michaels,Ruiz, Francisco,Cichewicz, Robert H.,McHardy, Stanton F.,Mooberry, Susan L.
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p. 9275 - 9289
(2017/11/30)
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- Synthesis of (R)-tembamide and (R)-aegeline via asymmetric transfer hydrogenation in water
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The synthesis of (R)-tembamide and (R)-aegeline via asymmetric transfer hydrogenation involving enantioenriched monosulfonamide-RhCp a - complex in aqueous sodium formate as hydride donor is described.
- Cortez, Norma A.,Aguirre, Gerardo,Parra-Hake, Miguel,Somanathan, Ratnasamy
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p. 1297 - 1302
(2013/11/19)
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