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)]