Total Synthesis of Complestatin (Chloropeptin II)

Complestatin was isolated in 1980 from the mycelium of Streptomyces lavendulae as inhibitor of alternative pathways to the complement cascade. An efficient synthesis of complestatin was developed. Intramol. Suzuki-Miyaura and SNAr reactions were employed for the construction of two macrocycles by the formation of aryl-aryl and aryl-aryl ether bonds, resp. A [3+3] segment coupling was used for the construction of the hexapeptide backbone, which makes this synthesis highly convergent. [on SciFinder (R)]