This review provides an overview of recent developments in Citrus aurantium L. (sour or bitter orange), focusing on its bioactive compounds, innovative extraction techniques, and technological applications. C. aurantium is rich in bioactive compounds such as flavonoids (naringin, hesperidin, kaempferol, quercetin), essential oils (β-pinene, limonene), and vitamin C, which represents significant biological activities including antioxidant, antimicrobial, anti-inflammatory, and anticancer effects. The review discusses traditional extraction methods, such as solvent extraction and hydrodistillation, alongside newer, eco-friendly approaches like ultrasound-assisted extraction, microwave-assisted extraction, supercritical fluid extraction, and natural deep eutectic solvents. It also highlights cutting-edge techniques, including molecular imprinting polymer-based extraction, which enable the more efficient enrichment and purification of specific compounds like synephrine. Finally, the review examines the diverse industrial applications of these bioactive compounds in sectors such as foods, pharmaceuticals, and cosmetics, while emphasizing the growing need for sustainable and efficient extraction technologies.