Avermectins were isolated as compounds possessing anthelmintic activity from the culture broth of Streptomycesavermitilis by Ōmura and co-workers. Owing to their potent anthelmintic and insecticidal activities, as well as their unique pentacyclic architecture, the avermectin family attracted keen interest from synthetic organic chemists. We have recently completed a more efficient and straightforward total synthesis of avermectin B1a, as compared with previous syntheses.