The panorama of natural synthesis has modified within the final twenty years, particularly in areas reminiscent of pharmaceutical synthesis and large-scale industrial synthesis. The progress and improvement of artificial methodologies along with an rising consideration to environmental and security issues, has led many researchers to check procedures that could possibly be suitable with a sustainable improvement of business manufacturing. Till few years in the past, the manufacturing of API’s was considerably dominated by a dependable and strong chemistry however which however presents some criticisms from the standpoint of the size of the artificial procedures by way of steps, and subsequently by way of waste manufacturing. In recent times, nonetheless, we now have been witnessing the adoption, even by giant industrial teams, of step-economical methodologies based mostly on direct C─H functionalization reactions, that in comparison with reactions reminiscent of cross-coupling or fragrant nucleophilic substitutions, they promise a greater sustainaibility as they don’t require pre-functionalized substrates, and subsequently supply the intruiguing risk for decreasing the variety of steps to acquire the goal. This assessment presents exemplary case research analyzed holistically on the premise of waste manufacturing (E-factor) and on the premise of environmental and security hazard scores (ES and SHS scores) with the intention of quantifying whether or not the adoption of direct C─H functionalization expertise is definitely at all times the best technique in comparison with basic approaches. Subsequently, finally give the reader a quantitative analysis on how is definitely promising by way of sustainability the present course of chemical manufacturing in comparison with earlier methodologies.