Cannabis sativa and related plants are recognized for their psychoactive and therapeutic effects due to the unique molecules they produce, including phytocannabinoids. Beyond the major phytocannabinoids Δ⁹-tetrahydrocannabinol and cannabidiol, research on ‘minor cannabinoids’ has revealed new biological properties, motivating alternative production methods for these low-abundance molecules. Advances in asymmetric synthetic methods have enabled access to structurally complex cannabinoids and analogs. In tandem, synthetic biology approaches, including heterologous pathway reconstruction and functionally analogous enzyme discovery, have expanded the biosynthetic toolkit, delivering rare and novel cannabinoids at increasing scale. Here, we summarize the latest insights into cannabinoid pharmacology, synthetic chemistry innovations, and engineered production strategies, underscoring how feedback across disciplines is reshaping access to and understanding of minor cannabinoids.