Abstract We report herein the approach to the key advanced intermediate in the synthesis of the bioactive marine natural product dragmacidin D. By employing a modular synthesis strategy of three fragments (5, 7, and 8), the advanced intermediate 3 has been successfully synthesized in 2.5% yield over 15 steps by starting from nitrotoluene 20. The synthesis also involves sequential cross-coupling reactions, namely Sonogashira and Suzuki–Miyaura ...
