- Diaryliodoniums by Rhodium(III)-Catalyzed C-H Activation: Mild Synthesis and Diversified Functionalizations
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Diaryliodonium salts play an increasingly important role as an aryl source. Reported is the first synthesis of diaryliodoniums by rhodium(III)-catalyzed C-H hyperiodination of electron-poor arenes under chelation assistance. This C-I coupling reaction occurred at room temperature with high regio-selectivity and functional-group compatibility. Subsequent diversified nucleophilic functionalization of a diaryliodonium allowed facile construction of C-C, C-N, C-O, C-S, C-P and C-Br bonds, and in all cases the initial functionalization occurred at the arene containing the chelating-group. Bonds aplenty: Diaryliodonium salts were synthesized for the first time from electron-poor arenes by the title reaction. The diaryliodoniums can be readily functionalized by nucleophiles with high chemoselectivity, thus leading to C-C, C-S, C-N, C-P, and C-Br bond formation. Cp=C5Me5, DG=directing group, Ts=4-toluenesulfonyl.
- Xie, Fang,Zhang, Zhipeng,Yu, Xinzhang,Tang, Guodong,Li, Xingwei
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- DIAMIDE MACROCYCLES AS FACTOR XIA INHIBITORS
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The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
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(2017/01/02)
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