Alternariol (1) and alternariol-9-methyl ether (1a) are major toxins produced by Alternaria species (Fig. 1). Owing to their ubiquitous occurrence as well as their ability to grow and produce toxins even under unfavorable conditions such as low temperature and low water activity, fungi of the genus Alternaria are sources of contamination in refrigerated fruits, vegetables, and stored feedstuffs. Toxins produced by Alternaria species have been encountered in corn flakes, cereals, fruits such as tomatoes and apples, and other crops. Exposure to Alternaria has also been associated with adverse health effect. For example, cereals contaminated with high amounts of Alternaria have been reported to be related to an enhanced incidence of esophageal cancer in China. Alternariol (1) and alternariol-9-methyl ether (1a) have been isolated from infected fruits in submilligram amounts. However, larger quantities of these of these compounds are needed if we are to achieve a detailed understanding of their formation, biosynthesis and metabolism; such knowledge is needed in order to minimize crop losses and toxicological residual risks. Despite this need, the effective synthetic methods for these compounds have yet to be developed. Although the preparation of 1 from 1a was reported in the early 1960s, 1a was obtained as the major side-product during the total synthesis of 1. By modifying the reported convergent strategy via the Suzuki-type formation of the biaryl moiety, we hereby report the total synthesis of alternariol 1 in high yields without the generation of its side-product 1a.