Indoles and their derivatives have dominated a significant proportion of nitrogen‐containing heterocyclic compounds and play an essential role in synthetic and medicinal chemistry, pesticides, and advanced materials. Compared with conventional synthetic strategies, direct functionalization of indoles provides straightforward access to construct diverse indole scaffolds. As we enter an era emphasizing green and sustainable chemistry, utilizing environment‐friendly solvents represented by water demonstrates great potential in synthesizing valuable indole derivatives. This review aims to depict the critical aspects of aqueous‐mediated indoles functionalization over the past decade and discusses the future challenges and prospects in this fast‐growing field. For the convenience of readers, this review is classified into three parts according to the bonding modes (C−C, C−N, and C−S bonds), which focus on the diversity of indole derivatives, the prominent role of water in the chemical process, and the types of catalyst systems and mechanisms. We hope this review can promote the sustainable development of the direct functionalization of indoles and their derivatives and the discovery of novel and practical organic methods in aqueous phase.
A series of multifunctional dihydroquinolinone frameworks have been synthesized via synergistic catalysis combining photolysis and Lewis base catalysis utilizing in situ generated ketenes from the visible-light-mediated Wolff rearrangement of α-diazoketones...
Targeted
protein degradation (TPD) technology is based on a unique
pharmacological mechanism that has profoundly revolutionized medicinal
research by overcoming limitations associated with traditional small-molecule
drugs. Autophagy, a mechanism for intracellular waste disposal and
recovery, is an important biological process in medicinal research.
Recently, studies have demonstrated that several emerging autophagic
degraders can treat human diseases. Herein we summarize the progress
in medicinal research on autophagic degraders, including autophagosome-tethering
compounds (ATTEC), autophagy-targeting chimeras (AUTAC), and AUTOphagy-TArgeting
chimeras (AUTOTAC), for treating human diseases. These autophagic
degraders exhibit excellent potential for treating neurodegenerative
diseases. Our research on autophagic degraders provides a new avenue
for medicinal research on TPD via autophagy.
Light is a fundamental energy source that has considerably driven scientific progress, especially in the fields of synthetic chemistry and pharmaceuticals. Visible-light-mediated synthetic chemistry has revolutionized conventional bond formation and...
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