Synthetic Studies on Dragmacidin D: Synthesis and Assembly of Three Fragments Towards an Advanced Intermediate

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 reactions, so that various analogues can be efficiently synthesized, which will allow the study of structure–activity relationships of dragmacidin D.