Concise total synthesis of antiarrhythmic drug dronedarone via a conjugate addition followed intramolecular heck cyclization,Journal of Heterocyclic Chemistry

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Concise total synthesis of antiarrhythmic drug dronedarone via a conjugate addition followed intramolecular heck cyclization
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2021-06-04 , DOI: 10.1002/jhet.4316
Sai Reddy Doda ₁ , Madhu Madasu ₁ , Prem Kumar Begari ₁ , Krishna Rao Dasari ₁ , Gangadhar Thalari ₂ , Sudhakar Kadari _{2,

3} , J. S. Yadav _{1,

4}

Affiliation

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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