Abstract: In modern discovery of innovative drugs, the quality of compound library directly affects the success of the whole process of research and development. Thus, how to quickly construct a high-quality library of compounds large in number and rich in structural diversity is a key step in drug discovery. With the rapid development of miniaturized (microscale/nanoscale) synthetic technology and biological screening technology, the goal of constructing multiple high quality compound libraries in a short time has been gradually realized, new hit and lead compounds being constantly discovered. Based on the relevant research in recent years, the latest progress in drug discovery through nanoscale synthesis is summarized, aiming to provide new insights to drug discovery based on miniaturized synthesis.