The Schmidt reaction has been an efficient and widely used synthetic approach to amides and nitriles since its discovery in 1923. However, its application often entails the use of volatile, potentially explosive, and highly toxic azide reagents. Here, we report a sequence whereby triflic anhydride and formic and acetic acids activate the bulk chemical nitromethane to serve as a nitrogen donor in place of azides in Schmidt-like reactions. This protocol further expands the substrate scope to alkynes and simple alkyl benzenes for the preparation of amides and nitriles.

The electrophilic halogenation of arenes is perhaps the simplest method to prepare aryl halides, which are important structural motifs in agrochemicals, materials, and pharmaceuticals. However, the nucleophilicity of arenes is weakened by the electron-withdrawing substituents, whose electrophilic halogenation reactions usually require harsh conditions and lead to limited substrate scopes and applications. Therefore, the halogenation of arenes containing electron-withdrawing groups (EWGs) and complex bioactive compounds under mild conditions has been a long-standing challenge. Herein, we describe Brønsted acid-catalyzed halogenation of arenes with electron-withdrawing substituents under mild conditions, providing an efficient protocol for aryl halides. The hydrogen bonding of Brønsted acid with the protic solvent 1,1,1,3,3,3-hexafluoro-2-propanol (HFIP) enables this transformation and thus solves this long-standing problem.

Alzheimer’s disease (AD) is one of the most challenging diseases around the world with no effective clinical treatment. Previous studies have suggested c-Jun N-terminal kinase 3 (JNK3) as an attractive therapeutic target for AD. Herein, we report 3-substituted indolin-2-one derivatives as the first isoform-selective JNK3 inhibitors by multistage screening. In this study, comparative structure-based virtual screening was performed, and J30-8 was identified with a half-maximal inhibitory concentration of 40 nM, which exhibited over 2500-fold isoform selectivity and marked kinome-wide selectivity. Further study indicated that 1 μM J30-8 exhibited neuroprotective activity in vitro so as to alleviate the spatial memory impairment in vivo through reducing plaque burden and inhibiting the phosphorylation of JNKs, Aβ precursor protein, and Tau protein. All of these indicated J30-8 as proved isoform-selective JNK3 inhibitors that might serve as a useful tool for further JNK3 studies with AD as well as for the development of JNK3 inhibitors for the potential treatment of neurodegenerative diseases.

Nowadays, the international community is becoming increasingly concerned about the sustainable utilization of natural resources. In order to protect the environment and reward sustainable practices, eco-labeling that signifies the environmental friendliness of the labeled food is already widely promoted in many regions around the world. Thus, it is of great importance for researchers to study consumers’ attitudes toward eco-labeled food as food is supposed to satisfy consumers’ needs. This study employed the event-related potentials (ERPs) approach to investigate consumers’ attitudes toward eco-labeled food by comparing their neural processing of visual stimuli depicting eco-labeled and non-labeled food. Our results showed that behaviorally, participants preferred to buy eco-labeled food rather than non-labeled one. At the neural level, we observed markedly smaller P2 and N2 amplitudes when pictures of eco-labeled food were presented. Furthermore, we also found that amplitudes of P2 were negatively correlated with participants’ purchase intention. Therefore, our current findings suggest that, while the environmental-friendly eco-labeling was not to one’s own interests, it might still be evocative, which induce consumers’ positive emotion, bring less cognitive conflict to the purchase decision-making and then result in a greater purchasing intention. This effect might be the result of the delivered value of social desirability.

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