Licochalcone A (LA), a useful and valuable flavonoid, is isolated from Glycyrrhiza uralensis Fisch. ex DC. and widely used clinically in traditional Chinese medicine. We systematically updated the latest information on the pharmacology of LA over the past decade from several authoritative internet databases, including Web of Science, Elsevier, Europe PMC, Wiley Online Library, and PubMed. A combination of keywords containing “Licochalcone A,” “Flavonoid,” and “Pharmacological Therapy” was used to help ensure a comprehensive review. Collected information demonstrates a wide range of pharmacological properties for LA, including anticancer, anti-inflammatory, antioxidant, antibacterial, anti-parasitic, bone protection, blood glucose and lipid regulation, neuroprotection, and skin protection. LA activity is mediated through several signaling pathways, such as PI3K/Akt/mTOR, P53, NF-κB, and P38. Caspase-3 apoptosis, MAPK inflammatory, and Nrf2 oxidative stress signaling pathways are also involved with multiple therapeutic targets, such as TNF-α, VEGF, Fas, FasL, PI3K, AKT, and caspases. Recent studies mainly focus on the anticancer properties of LA, which suggests that the pharmacology of other aspects of LA will need additional study. At the end of this review, current challenges and future research directions on LA are discussed. This review is divided into three parts based on the pharmacological effects of LA for the convenience of readers. We anticipate that this review will inspire further research.

Visible-light-mediated sequential Wolff rearrangement and Staudinger cycloaddition for the assembly of valuable spiro-pyrazolone-β-lactams for the first time is disclosed by utilizing in situ generated ketenes and pyrazolone ketimines. This powerful approach features high yield, good substrate tolerance, and gram-scale capacity, and provides straightforward access to multisubstituted pyrazole-morpholine skeletons. The control experiments indicate that visible-light-mediated irradiation plays an essential role in the cyclization process, and a plausible mechanism is proposed to explain the observed efficiency.

A catalytic asymmetric construction of the bispiro[pyrazolone-dihydropyrrole-oxindole] skeleton catalyzed by chiral DMAP-derived catalyst was successfully achieved by employing recently explored pyrazolone-derived MBH carbonate.

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 enabled previously inaccessible chemical processes under mild conditions. However, the continuous consumption of photocatalysts and corresponding additives has led to system complexity and cost escalation, making the development of photoactivated substrates a promising yet challenging research frontier. Recently, emerging photogenerated ketenes as a potent class of organic compounds has provided a promising solution to the challenges associated with classic ketene preparation and application, with reduced preparative costs and simplified processes. This review highlights how photogenerated ketenes have simplified and accelerated the synthesis of diverse cyclic architectures through [2 + n] cyclization reactions and complex natural products through Danheiser benzannulation. Significantly, their successful application in flow chemistry has demonstrated remarkable potential for industrialization. Despite challenges in terms of limited cyclic architectures, elusive mechanisms, and challenging chiral control, ongoing efforts in investigating the chemical behaviors of photogenerated ketenes and exploring their potential applications hold promise for breakthrough discoveries, propelling the field forward sustainably.

The direct functionalization of inert C–H bonds is regarded as one of the most powerful strategies to form various chemical bonds and construct complex structures. Although significant advancements have been witnessed in the area of transition metal-catalyzed functionalization of inert C–H bonds, several challenges, such as the utilization and removal of expensive transition metal complexes, limited substrate scope and large-scale capacity, and poor atom economy in removing guiding groups coordinated to the transition metal, cannot fully fulfill the high standard of modern green chemistry nowadays. Over the past decades, due to its inherent advantage compared with a transition metal-catalyzed strategy, the hydride shift activation that applies “tert-amino effect” into the direct functionalization of the common and omnipresent C(sp³)–H bonds adjacent to tert-amines has attracted much attention from the chemists. In particular, the intramolecular [1,5]-hydride shift activation, as the most common hydride shift mode, enables the rapid and effective production of multifunctionally complex frameworks, especially the spiro-tetrahydroquinoline derivatives, which are widely found in biologically active natural products and pharmaceuticals. Although great accomplishments have been achieved in this promising field, rarely an updated review has systematically summarized these important progresses despite scattered reports documented in several reviews. Hence, in this review, we will summarize the significant advances in the cascade [1,5]-hydride shift/intramolecular C(sp³)-H functionalization from the perspective of “tert-amino effect” to build a spiro-tetrahydroquinoline skeleton, and the content is categorized by structure type of final spiro-tetrahydroquinoline products containing various pharmaceutical units. Besides, current limitations as well as future directions in this field are also pointed out. We hope our review could provide a quick look into and offer some inspiration for the research on hydride shift strategy in the future.