Abstract To accomplish the United Nation's primary Sustainable Development Goals (SDGs), particularly SDG 3: good health and well‐being and SDG 9: industry, innovation, and infrastructure, it is essential to develop synthesis processes that are sustainable, cost‐effective, and environmentally friendly. These processes should enable the efficient and non‐toxic total synthesis of various drugs and natural products while minimizing impurities. This can be accomplished using inexpensive catalysts and reagents, such as zinc and its salts. This review compiles recent advancements in the field of total synthesis of bioactive natural products and active pharmaceutical molecules, encompassing the literature from the past two decades and highlighting the importance of zinc metal and its relative components in promoting a broad range of organic transformations. Like organo‐zinc mediated transformations, zinc‐mediated reductive elimination/cleavage, zinc chloride, zinc metal, zinc triflate, zinc bromide‐mediated transformations, and zinc perchlorate‐mediated epoxide ring opening are categories in this review.