Abstract: Carolyn R. Bertozzi, Morten Meldal, and K. Barry Sharpless received the 2022 Nobel Prize in Chemistry, attributed to their study on click chemistry and bioorthogonal chemistry. Click chemistry aims to rapidly and reliably synthesize various molecules by linking small units, while bioorthogonal reactions apply this to specially label and visualize living systems without interfering the biological surrounding. “Precise synthesis” has been introduced into the human body, enabling the clinical translation of “drug synthesis in vivo” and “3D bioprinting of tissues in vivo”. Therefore, click chemistry that started with organic chemistry have been widely applied in cancer therapy. The applications of click chemistry and bioorthogonal chemistry in precise imaging, targeted therapy, genetic engineering, and viral vaccines are summarized in this work. The practical application of personalized medicine, new drug research and development, and regenerative medicine are constantly promoted.