The intrinsic limitations of conventional batch synthesis have hindered its applications in both solving classical problems and exploiting new frontiers. Microfluidic technology offers a new platform for chemical synthesis toward either molecules or materials, which has promoted the progress of diverse fields such as organic chemistry, materials science, and biomedicine. In this review, we focus on the improved performance of microreactors in handling various situations, and outline the trend of microfluidic synthesis (microsynthesis, μSyn) from simple microreactors to integrated microsystems. Examples of synthesizing both chemical compounds and micro/nanomaterials show the flexible applications of this approach. We aim to provide strategic guidance for the rational design, fabrication, and integration of microdevices for synthetic use. We critically evaluate the existing challenges and future opportunities associated with this burgeoning field.