Abstract
Indole derivatives are among the most useful and interesting heterocycles employed in drug discovery and medicinal chemistry. In addition, flow chemistry and flow technology are changing the synthetic paradigm in the field of modern synthesis. In this review, the role of flow technology in the preparation of indole derivatives is showcased. Selected examples have been described with the aim to provide readers with an overview on the tactics and technologies used for targeting indole scaffolds.
Highlights
Among heterocycles, the indole ring is one of the most ubiquitous in nature as well as in man-made products, such as pharmaceuticals, agrochemicals, dyes, and materials [1,2]
Approach applied to Fischer indole synthesis: (a) first example proposed by Bagley; (b) nonresonant microwave system for continuous flow synthesis developed by Larhed; (c)
The relevance of indole, a biologically accepted pharmacophore compounds, and its have tried to report the contribution of flow chemistry in the reinforcement of synthetic strategies for derivatives, requires a continuous improvement of their preparation
Summary
The indole ring is one of the most ubiquitous in nature as well as in man-made products, such as pharmaceuticals, agrochemicals, dyes, and materials [1,2]. The indole core appears as a substructure of various biologically active compounds, including the neurotransmitter serotonin; the regulatory hormone melatonin; and various medicines, such as antihypertensive, anti-inflammatory, antimigraine, anti-tumor, and many others (Scheme 1) [3]. Indole is a privileged scaffold in drug discovery programs targeting new antivirals. Examples of marketed indole-containing antiviral drugs include Arbidol and Delavirdine. Arbidol is used for the treatment and prophylactic prevention of influenza A and B virus and SARS. Molecules 2020, 25, x FOR PEER REVIEW of 28 non-nucleoside reverse transcriptase inhibitor that was approved by the FDA in 1997 for the treatment review, recent flow chemistry approaches developed for strengthening the tactics of indole ring of human immunodeficiency virus type 1 (HIV-1) [4,5]. Selected examples of indole-containing biologically active compounds
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