An asymmetric hydrosilylation of 2,2-difluoro-1,3-diketones was successfully realized by using a frustrated Lewis pair of chiral borane and tricyclohexylphosphine as a catalyst to give a variety of α,α-difluoro-β-hydroxyketones in high yields with up to 99% ee.

Comprehensive Summary

The asymmetric partial reduction of 1,3-diketones stands as a straightforward pathway to access optically active β-hydroxyketones. In this paper, an asymmetric Piers-type hydrosilylation of 2,2-difluoro-1,3-diketones was successfully realized by using a frustrated Lewis pair of chiral borane and tricyclohexylphosphine as a catalyst, delivering a variety of α,α-difluoro-β-hydroxyketones in high yields with up to 99% ee. Significantly, no over-reduced diol products were observed even with an excess amount of silanes. The product can be conveniently converted to α,α-difluoro-β-hydroxyester or 1,3-anti-diol via an oxidation with m-CPBA or a reduction with DIBAL-H without obvious loss of ee.

2-Aminobenzothiazoles derivatives have revealed a broad spectrum of biological activities, such as anti-HIV, anti-inflammatory, antioxidant, anti-microbial, anti-tumour, anti-infective, and anti-convulsant activities. A great amount of 2-aminobenzothiazole derivatives have been applied in drugs for the treatment of human diseases. A convenient approach for the construction of 2-aminobenzothiazoles via I₂-catalyzed tandem cyclization reaction of amines and carbon disulfide has been developed. More details are discussed in the article by Deng et al. on page 846—852.

2-Aminobenzothiazoles derivatives have revealed a broad spectrum of biological activities, such as anti-HIV, anti-inflammatory, antioxidant, anti-microbial, anti-tumour, anti-infective, and anti-convulsant activities. A great amount of 2-aminobenzothiazole derivatives have been applied in drugs for the treatment of human diseases. A convenient approach for the construction of 2-aminobenzothiazoles via I₂-catalyzed tandem cyclization reaction of amines and carbon disulfide has been developed. More details are discussed in the article by Deng et al. on page 846—852.

A Ni(II)-catalyzed asymmetric difunctionalization of alkynes is reported. This method involves intermolecular regioselective arylation of the alkynes and intramolecular desymmetrization of dinitriles, enabling the synthesis of enantioenriched azepine derivatives. The reaction exhibits good tolerance toward various functional groups, resulting in high yields and enantioselectivities.

Comprehensive Summary

The azepine ring is a prominent structural scaffold in biologically significant molecules. In this study, we present a Ni(II)-catalyzed asymmetric difunctionalization of alkynes, involving intermolecular regioselective arylation and intramolecular nitrile addition, enabling the synthesis of enantioenriched azepine derivatives. This reaction simultaneously installs an all-carbon quaternary stereocenter and introduces an unprotected imine functionality, showing great promise for subsequent transformations. The reaction exhibits good tolerance toward various functional groups, resulting in high yields and enantioselectivities. The synthetic utility of this methodology is further demonstrated through gram-scale synthesis and product derivatization. This research offers an efficient approach to the synthesis of seven-membered nitrogen heterocycles.

Palladium-catalyzed dipolar [4+2] and [6+2] cycloaddition reactions of benzo[d]isothiazole 1,1-dioxides (BDs) have been developed for the construction of of BD-fused 1,3-oxazinanes and 1,3-oxazocanes derivatives, respectively.

Comprehensive Summary

The Pd-catalyzed dipolar cycloaddition represents a significant synthetic strategy for the construction of useful heterocyclic compounds. This study developed the dipolar [4+2] and [6+2] cycloaddition reactions of benzo[d]isothiazole 1,1-dioxides (BDs) leading to the synthesis of BD-fused 1,3-oxazinane and 1,3-oxazocane derivatives, respectively. In particular, the synthesis of BD-fused 1,3-oxazinanes demonstrated regio- and enantioselective characteristics, resulting in products with good yields, enantioselectivity and regioselectivity (if applicable). Furthermore, the [6+2] cycloaddition reaction developed in this work represented the first strategy for the synthesis of medium-sized ring compounds based on BDs.

Azepine ring is a prominent structural scaffold in biologically significant molecules. This study demonstrates a Ni(II)-catalyzed alkyne functionalization/cyclization cascade reaction of alkyne-tethered malononitriles, involving intermolecular regioselective arylation of the alkynes and desymmetrizing addition onto the nitrile group, to access azepine derivatives. This strategy introduces an all-carbon quaternary stereocenter and an unprotected imine functionality simultaneously to the azepine scaffold, showing great promise for subsequent transformations. More details are discussed in the article by Liu et al. on page 873—878.

Azepine ring is a prominent structural scaffold in biologically significant molecules. This study demonstrates a Ni(II)-catalyzed alkyne functionalization/cyclization cascade reaction of alkyne-tethered malononitriles, involving intermolecular regioselective arylation of the alkynes and desymmetrizing addition onto the nitrile group, to access azepine derivatives. This strategy introduces an all-carbon quaternary stereocenter and an unprotected imine functionality simultaneously to the azepine scaffold, showing great promise for subsequent transformations. More details are discussed in the article by Liu et al. on page 873—878.

Comprehensive Summary

Eight rare capnosane-type cembranoids, sarcocinerenoids A—H (1—8) and two new cage-type cembranoids sarcocinerenoids I—J (9—10) were isolated from the soft coral Sarcophyton cinereum. The 5/11 bicyclic carbon skeleton is the same in Sarcocinerenoids A—H (1—8), and they collocate distinctive oxygen rings. Sarcocinerenoids I—J (9—10) with a cage-type structure have been discovered to have an oxygen bridge and an uncommon seven-membered ring. Extensive spectroscopic investigation, X-ray diffraction analysis, estimated ECD, and DP4+ probability assessments were used to ascertain the structures of the two types of diterpenoids. Moreover, compounds 1, 4 showed promoting angiogenesis activity in zebrafish assays.

The bifunctional fluorescent probe Mito-Q can not only effectively detect mitochondrial viscosity changes and mitophagy, but also be successfully applied to observe the fusion of mitochondrial-containing autolysosomes and autophagosomes (FMAA).

Comprehensive Summary

Autophagy is a multi-step cell metabolism process in which cells remove damaged and unwanted materials. During autophagy, autophagosomes fuse with lysosomes to form autophagosomes. Autophagosomal membrane components are recycled from autolysosomes through the autophagosomal components recycling (ACR), while lysosomal components circulate on the autolysosomal surface through the autophagic lysosome reformation (ALR) process. Autolysosomes contain components from autophagosomes and lysosomes. However, whether there is a fusion between autolysosome and autophagosome or lysosome at the organelle level remains unknown. In this study, a pH and viscosity dual-controlled mitochondria-targeting fluorescent probe Mito-Q was designed based on an asymmetric norcyanine to achieve the high-contrast imaging of mitochondria-containing autolysosomes. Mito-Q not only effectively detected mitochondrial viscosity changes and mitophagy with high sensitivity, but more importantly, the fusion of mitochondria-containing autolysosomes and autophagosomes (FMAA) was observed during autophagy by the real-time confocal imaging of HeLa cells.

As classic molecular magnets with magnetic bistability, spin-crossover (SCO) compounds have potentially important application value in molecular electronics, sensing, and information storage. Multistable control of SCO compounds is more difficult than bistability control. In this paper, we propose a strategy to control the number of spin-transition steps to further understand the control of the multistability of SCO compounds. More details are discussed in the article by Li et al. on page 879—886.

As classic molecular magnets with magnetic bistability, spin-crossover (SCO) compounds have potentially important application value in molecular electronics, sensing, and information storage. Multistable control of SCO compounds is more difficult than bistability control. In this paper, we propose a strategy to control the number of spin-transition steps to further understand the control of the multistability of SCO compounds. More details are discussed in the article by Li et al. on page 879—886.