Baicalin is the most abundant ingredient of Scutellaria baicalensis, which has been shown to have a variety of biological activities. In this study, we have developed an efficient synthetic route for this compound based on Koenigs-Knorr glycosylation and mild-basic deprotection. Through this route, baicalin was obtained from cheap starting materials in a linear longest 10-step sequence with an overall yield of 27%. Four analogs of baicalin were also synthesized in high yields with the key protocols developed in the synthesis of baicalin, demonstrating the general applicability of our synthetic route. Efficient synthesis of baicalin and its analogs will hopefully facilitate further structure-activity relationship studies of this class of compounds. (C) 2015 Elsevier Ltd. All rights reserved.