Heterocycles are a valuable type of structural motifs which occupy a major space in the area of medicinal, pharmaceutical, and bioactive natural product chemistry as well as synthetic organic chemistry. Most frequently, nitrogen heterocycles represent a highly significant type of compounds that are extensively employed in agrochemistry, materials science, and synthesis of bioactive complex molecules and it also has a profound role in modern drug design. Among N-heterocycles, bioactive N, Nheterocycles play a crucial role in the drug discovery and development process. Benzimidazoles, oxadiazoles, pyrazoles, pyrazolines, pyridazines, pyrimidines, thiadiazoles, triazoles, etc. are important classes of N, N-heterocycles due to their significant physiological and biological activities as well as versatile synthetic utility. For example, compounds containing an oxadiazole core such as phidianidines A and B display cytotoxicity. Zibotentan including 1,3,4-oxadiazole and pyrazine skeletons was accepted for the treatment of prostate cancer by the FDA, and cefozopran (SCE-2787) comprising 1,2,4-thiadiazole core is a powerful commercial antibiotic. So, there is continuing considerable attention to the improvement of efficient, convenient, and eco-friendly synthetic protocols for the formation of pharmaceutically relevant N,N-heterocycles. In this context, visible light-assisted synthesis of bioactive N,N-heterocycles has a great impact on sustainable development as it constitutes a clean, renewable, and abundant energy source, as well as its encouraging application in industry. Hence, this review aims to deal with the understanding of the visible light-promoted synthesis of bioactive N,N-heterocycles and further stimulate the development of more new relevant strategies.