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Microwave-Assisted Synthesis of Medicinally Relevant Indoles

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Indoles represent an important structural class in medicinal chemistry with broad spectrum of biological activities. The synthesis of indoles, therefore, has attracted enormous attention from synthetic chemists. Microwave methods for the preparation of indole analogs have been developed to speed up the synthesis, therefore, microwave assisted organic synthesis (MAOS) in controlled conditions is an invaluable technique for medicinal chemistry. In this review, indole forming classical reactions such as Fischer, Madelung, Bischler-Mohlau, Batcho-Leimgruber, Hemetsberger-Knittel, Graebe-Ullmann, Diels-Alder and Wittig type reactions using microwave radiation has been summarized. In addition, metal mediated cyclizations along with solid phase synthesis of indoles have been discussed.

Keywords: AstraZeneca; Batcho-Leimgruber; Bischler-Mohlau; Diels-Alder; Fischer; Fischer indole; Frovatriptan; Glaxo; Graebe-Ullmann; Hemetsberger-Knittel; Indole alkaloid cryptosanguinolentine; Indoles; Madelung; Microwave irradiation; Microwave-assisted solid-phase or-ganic synthesis (MASPOS); Sonogashira; Sumatriptan; Transition metal; Vernalis; Wittig type; Zolmitriptan; antibiotic indolmy-cin; cyclizations; green chemistry; non-steroidal anti-inflammatory; one-pot synthesis; serotonin; solid phase organic synthesis; synthesis (MAOS); tryptophan

Document Type: Research Article


Publication date: February 1, 2011

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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