Currently, the treatment for HBV infection suffers from adverse side effects and drug resistance. The dramatic development of new HBV inhibitors is focused on discovering diverse non-nucleoside compounds with either novel structures or new mechanisms of action. Capsid assembly is crucial to the completion of the viral life cycle, which makes it an attractive target for antivirus discovery. Inhibitors that block the formation of the HBV capsid have been developed, and several candidates have been proposed. In this review, we focus on the recent advances in several distinct classes of synthetic small molecular non-nucleosides targeting at the capsid assembly.