- Radical-mediated divergent cyclization of benzamides toward perfluorinated or cyanated isoquinolinediones
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A simple and efficient copper-controlled divergent cyclization of benzamides, which leads to perfluorinated or cyanated isoquinolinediones, is developed. In the presence of AIBN, methacryloyl benzamides with perfluoroalkyl iodides undergo cascade radical addition/cyclization to afford perfluoroinated isoquinolinediones as the major product under metal-free conditions, whereas the use of CuI (10 mol%) is able to redirect the cyclization to yield isoquinolinediones bearing an α-cyano quaternary carbon center. The cyclization features controllable divergent synthesis and a broad substrate scope as well as highly practical reaction conditions, thereby making this strategy a highly attractive means to fluorinate or cyanate isoquinolinediones.
- Deng, You-Lin,Tang, Shi,Ding, Guo-Liang,Wang, Ming-Wei,Li, Jie,Li, Zeng-Zeng,Yuan, Li,Sheng, Rui-Long
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supporting information
p. 9348 - 9353
(2016/10/13)
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- 11a-Methano-TXA compounds
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The present invention provides novel 11a-methano-TXA compounds and intermediates and processs for their preparation. Further provided are methods for using these novel TXA analogs as inhibitors of thromboxane synthetase, rendering these analogs useful for a variety of pharmacological purposes. These pharmacological uses include anti-inflammatory, anti-thromobitc, and anti-asthma indications.
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