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Green chemistry is a fascinating research area due to its respect to environment and effectiveness for more purified organic compounds, which will be active pharmaceuticals. Twelve principles of green chemistry should be obeyed, and these principles can manage the researchers to enhance productivity and reduce hazardous effects on human health. Active pharmaceutical ingredients (API) should have adequate purity due to their use in human health. Any contamination coming from adopted protocols can influence the product. These disadvantages increase further purification protocols, which led to using more power, chemicals, and increase product cost. All these disadvantages can be dropped using green chemistry principles. Around the world, pharmaceutical industries afford to do green protocol due to human health and product costs. These aims led them to find out new and greener synthetic protocols that can be utilized on an industrial scale. These protocols are imperative and can be transferred in research and development, which have been progressed in the university or other industries. In this chapter, we desire to exhibit the heart of green chemistry for pharmaceutical industries and show how they succeeded in green protocols. These protocols will be discussed in terms of their effectiveness and advantages in API. Opinion shows that green chemistry principles can save the cost of about 65.5 billion by 2020. The most direct and straightforward way to employ green chemistry in pharmaceuticals is to employ eco-friendly, nonhazardous, reproducible, and cost-effective solvents and catalysts in the synthesis of drug molecules and researches involving synthetic chemistry. Also, flow chemistry will be a powerful tool for the synthesis of API, as well.

N-Heterocycles are essential frameworks, mentioned in countless scientific works, that open a large gate into biologically active compounds; they are mentioned in medicinal chemistry as vital scaffolds. N-Heterocycles can be synthesized via many pathways, especially catalytic reactions that favor green chemistry principles. In catalytic approaches, copper has received special attention from scientists since it is more abundant than other metals, has lower toxicity, and can be handled easily. Copper-catalyzed cyclization reactions serve in many scientific fields, and these reactions resulting in N-heterocycles are of particular interest to the pharmaceutical industry, because many active medicinal ingredients can be synthesized using different copper catalysts. The importance of copper and its support in the synthesis of N-heterocycles was the impetus behind this chapter, and many examples are given of the synthesis of N-heterocycles in which copper catalysts were used. The presence of amine- and phosphine-based ligands for different selectivities, total synthesis using copper, synthesis of pharmaceutical products on gram scale, and biological activities of the mentioned N-heterocycles are all discussed in this chapter.