This review firstly covers the applications of 2-arylbenzothiazoles as amyloid imaging agents, antitumor agents, and organic luminescent materials. Then we review the recent advances in the synthesis of 2-arylbenzothiazole derivatives. On the one hand, we introduce the approaches for construction of the 2-arylbenzothiazole core, including the following categories: (i) classic condensation of 2-aminothiophenols, (ii) direct arylation of benzothiazoles, (iii) intramolecular cyclization of thiobenzanilides, and (iv) tandem cyclization of anilines/ nitroarenes­ with elemental sulfur or sulfides. On the other hand, the transition-metal-catalyzed direct C–H functionalizations of 2-aryl­benzothiazoles are also involved in this review.1 Introduction2 Applications of 2-Arylbenzothiazoles3 Construction of the 2-Arylbenzothiazole Core4 Synthesis 2-Arylbenzothiazoles via Direct C–H Functionalization5 Conclusion