Okitsu Takashi, Ogasahara Mizuki, Wada Akimori
Department of Organic Chemistry for Life Science, Kobe Pharmaceutical University.
Chem Pharm Bull (Tokyo). 2016;64(8):1149-53. doi: 10.1248/cpb.c16-00237.
We have developed a convergent synthesis of dronedarone, an antiarrhythmic agent. The key steps of the process are the construction of a benzofuran skeleton by iodocyclization and the carbonylative Suzuki-Miyaura cross-coupling for biaryl ketone formation. This synthetic route required only eight steps from 2-amino-4-nitrophenol in 23% overall yield.
我们已经开发出了一种用于合成抗心律失常药物决奈达隆的汇聚合成法。该过程的关键步骤是通过碘环化构建苯并呋喃骨架以及通过羰基化铃木-宫浦交叉偶联反应形成联芳基酮。这条合成路线从2-氨基-4-硝基苯酚出发仅需八步反应，总收率为23%。
