Concise total synthesis of antiarrhythmic drug dronedarone via a conjugate addition followed intramolecular heck cyclization |
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| Authors: | Madhu Madhasu Sai Reddy Doda Prem Kumar Begari Krishna Rao Dasari Gangadhar Thalari Sudhakar Kadari Jhillu Singh Yadav |
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| Institution: | 1. Department of Organic Synthesis & Process Chemistry, CSIR – Indian Institute of Chemical Technology, Hyderabad, India;2. Department of Chemistry, Osmania University, Hyderabad, India |
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| Abstract: | A concise, scalable, and an efficient total synthesis for dronedarone ( 2 ) was described using conjugate addition followed by intramolecular Heck cyclization. The other key reaction includes selective reduction of nitro functionality and addition of lithiated terminal alkyne to the aldehyde. The overall yield of this approach is 44% in six steps. |
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