Microwave assisted synthesis of medicinally relevant indole conjugates utilizing modified Hemetsberger-Knittel indole synthesis

• Online Access: http://hdl.handle.net/2047/D20211741

Indoles are a class of nitrogen containing heterocycles first synthesized by Bayer AG in 1866 that have a broad variety of biological activities. They have widely been recognized as a privileged scaffold and are best known for their medicinal properties in the pharmaceutical industry. The indole nucleus signifies a vast importance in the world as indoles are built into peptides, proteins, are the skeleton of many natural products, and are the core of many successful marketed drugs. To date over 10,000 unique indole derivatives have been discovered as being biologically active compounds due to their excellent binding affinity to various receptors. Upon entering the 21st century, drug discovery and development has experienced a lack of innovative ideas for new chemical entities. It is well known that the FDA has placed stricter safety, quality and efficacy regulations on pharmaceutical companies over the last few decades. This, coupled with long developmental processes and immense financial investments, has placed pharmaceutical companies in innovative strains regarding their small-molecule pipelines.