The Art of Total Synthesis of Bioactive Natural Products via Microwaves

Natural products are the most effective source of potential drug leads. The total synthesis of bioactive natural products plays a crucial role in confirming the hypothetical complex structure of natural products in the laboratory. The total synthesis of rare bioactive natural products is one of the great challenges for the organic synthetic community due to their complex structures, biochemical specificity, and difficult stereochemistry. Subsequently, the total synthesis is a long process in several cases, and it requires a substantial amount of time. Microwave irradiation has emerged as a greener tool in organic methodologies to reduce reaction time from days and hours to minutes and seconds. Moreover, this non-classical methodology increases product yields and purities, improves reproducibility, modifications of selectivity, simplification of work-up methods, and reduces unwanted side reactions. Such beneficial qualities have stimulated this review to cover the application of microwave irradiation in the field of the total synthesis of bioactive natural products for the first time during the last decade. An overview of the use of microwave irradiation, natural sources, structures, and biological activities of secondary metabolites is presented elegantly, focusing on the involvement of at least one or more steps by microwave irradiation as a green technique.

Automated summary

Natural products are important sources of potential drug leads, and total synthesis in the laboratory confirms complex structures but poses challenges due to complexity and stereochemistry. Microwave irradiation, a greener tool, reduces reaction time, increases product purities, improves reproducibility, simplifies work-up methods, and minimizes unwanted side reactions, sparking its application in the total synthesis of bioactive natural products.