Copper-catalysed radical cascade reaction of -(2-oxo-2-phenylethyl) substituted 2-pyridones with styrene to access 1,6-carboannulated 2-pyridone scaffolds.

Herein, we present that treating -(2-oxo-2-phenylethyl) substituted 2-pyridones with styrenes in DMSO/HO at 120 °C affords 1,6-carboannulated 2-pyridone scaffolds with up to 79% yield. This protocol provides a simple and efficient method for obtaining complicated bicyclic 2-pyridones through a radical cascade reaction. Additionally, we have successfully synthesized 27 target compounds, which confirms the practicality and wide applicability of the proposed reaction.

Electrochemical one-pot cascade synthesis of thio(seleno)cyanato-substituted thiazolidine-2-imines without external electrolyte.

A novel synthetic method has been developed for generating thio(seleno)cyanato-substituted thiazolidine-2-imines an electrochemical one-pot cascade reaction. This reaction employs isothiocyanates, -2-en-1-amines, and KSCN (or KSeCN) under mild conditions, obviating the need for metals, chemical oxidants, and external electrolytes. The protocol is effective with unactivated alkenes and facilitates the synthesis of five- and six-membered thio(seleno)cyanato-substituted thiazolidine-2-imines.

CuO-catalyzed cascade phosphinylation/cyclization of 2'-aminochalcones for the synthesis of hemi-indigo derivatives.

A CuO-catalyzed cascade phosphinylation/cyclization reaction of 2'-aminochalcones and diphenylphosphine oxides to produce hemi-indigo derivatives has been developed. This strategy facilitates the sequential formation of a C-P bonds and a C-N bond in a single reaction step. Notably, the approach features one-pot operation, an earth-abundant copper catalyst, readily available starting materials, a broad substrate scope and high compatibility with functional groups, providing 33 compounds in acceptable yields.

Palladium-Catalyzed (3 + 2) Annulation of Aromatic Acids by C(sp)-H Olefination and Decarboxylative Cross-Coupling Reaction.

A palladium-catalyzed (3 + 2) annulation of 2-methylbenzoic acid with maleimide using Ac-Leu-OH as a powerful ligand has been reported. Through a site-selective γ-C(sp)-H olefination reaction and a sequential decarboxylative cross-coupling reaction, a five-membered cyclic ring was obtained as the final product. This novel reaction features great site selectivity and reactivity to generate various cyclic products in moderate to good yields.

Corrigendum: Preclinical profiles of SKB264, a novel anti-TROP2 antibody conjugated to topoisomerase inhibitor, demonstrated promising antitumor efficacy compared to IMMU-132.

[This corrects the article DOI: 10.3389/fonc.2022.

The [3 + 2] Cycloaddition Reaction of -Substituted Pyrrole-2-carboxaldehydes with Arylalkenes under Copper Catalysis: Access to Dihydropyrrolizine Skeletons.

Herein, we found that treating -substituted pyrrole-2-carboxaldehydes with arylalkenes in DMF in N at 120 °C could afford pyrrolidine scaffolds with an up to 85% yield. This approach has several remarkable features, such as atom and step economy, readily accessible raw materials, and easy-to-operate manner, providing a simple and efficient method for constructing complicated bicyclic pyrroles. Additionally, we have successfully synthesized 28 target compounds, which further demonstrates its practicality and wide applicability.

Synthesis of β-Hydroxysulfides via Multi-Component Cascade Hydroxysulfenylation of Styrenes with NH SCN and Water under Transition-metal-free Conditions.

Transition-mental-free multi-component hydroxysulfenylation of styrenes with NH SCN and water to from β-hydroxysulfides is established. The reaction mechanism proceeded via a domino reaction after a radical addition to 2-phenylimidazo[1,2-a]pyridines. This approach features a wide substrate scope and functional group compatibility, providing 34 compounds in acceptable yields.

Synthesis of pyrazoles from sulfonyl hydrazone and benzyl acrylate under transition-metal-free conditions.

Pyrazoles as an important class of heterocyclic compounds, are widely found in pharmaceuticals and bioactive natural products. Herein we report a [3 + 2] cycloaddition reaction for the synthesis of a series of pyrazoles, with the yield up to 77%. This approach exhibits many notable features, such as convenient operating conditions, excellent functional group compatibility and readily accessible raw materials, providing an alternative route for the construction of pyrazole derivatives.

C-H Borylation of Benzophenones Using Hydrazone as the Traceless Directing Group.

C-H borylation is one of the powerful C-H bond functionalization reactions. In this context, a metal-free C-H borylation of benzophenones using hydrazone as the traceless directing group has been reported. The dibromoboron intermediates can be obtained in excellent yields, and the corresponding arylboronic esters are generated in moderate to excellent yields.

Palladium-Catalyzed Tandem Diolefination Reaction of Benzaldehyde Enabled by a Remote Directing Group.

A tandem diolefination reaction of benzaldehyde has been developed via Pd-catalyzed β-C(sp)-H olefination of the benzene ring and tandem C(sp)-H olefination of acrylate. 2-((Aminooxy)methyl)benzonitrile was involved with the benzaldehyde substrate as a remote directing group to realize the C-H bond activation. The control experiments proved that the presence of a remote cyano group is essential for this novel diolefination reaction.

Preclinical profiles of SKB264, a novel anti-TROP2 antibody conjugated to topoisomerase inhibitor, demonstrated promising antitumor efficacy compared to IMMU-132.

Purpose: The aim of this study was to improve the intratumoral accumulation of an antibody-drug conjugate (ADC) and minimize its off-target toxicity, SKB264, a novel anti-trophoblast antigen 2 (TROP2) ADC that was developed using 2-methylsulfonyl pyrimidine as the linker to conjugate its payload (KL610023), a belotecan-derivative topoisomerase I inhibitor. The preclinical pharmacologic profiles of SKB264 were assessed in this study.

Methods: The and pharmacologic profiles of SKB264, including efficacy, pharmacokinetics-pharmacodynamics (PK-PD), safety, and tissue distribution, were investigated using TROP2-positive cell lines, cell-derived xenograft (CDX), patient-derived xenograft (PDX) models, and cynomolgus monkeys.

Tandem C-C/C-N Bond Formation via Rh(III)-Catalyzed α-Fluoroalkenylation and Sequential Annulation of 2-Arylquinazolinones and -Difluorostyrenes.

An efficient method of Rh(III)-catalyzed coupling reaction between 2-arylquinazolinones and -difluorostyrenes has been developed. In this work, two diverse structures of monofluoroalkenes and isoindolo[1,2-]quinazolin-10(12)-one derivatives were respectively synthesized by controlling the amount of additives (Ca(OH) and AgNTf) to achieve controlled stepwise breaking of the C-F bonds of -difluorostyrenes. This reaction has the characteristics of a wide range of substrates and good functional group tolerance.

Adamantane-1-Carbonyl-Directed C-H Borylation and Hydroxylation of Benzenethiols.

A novel route has been described for C-H borylation and hydroxylation of benzenethiols directed by adamantane-1-carbonyl using BBr. The protocol generates corresponding arylboronic esters and phenols in moderate to excellent yields under metal-free conditions. In addition, the borylated product can be transformed and the directing group can be removed in good yields, which will facilitate the synthesis of structurally diverse benzenethiols.

Ligand-Enabled Sequential C(sp)-H and C(sp)-H Diolefination Reaction via Palladium Catalyst.

Palladium-catalyzed sequential C(sp)-H and C(sp)-H bond diolefination reaction of -toluidine has been realized for the first time using acetyl-protected aminoethyl phenyl thioether ligands. This novel reaction allows for preparation of the conjugated diene structure via an immediate second olefination on the basis of the first C(sp)-H olefination in one pot. Various triflyl-protected anilines and acrylates were used as coupling partners elegantly.

Metal-Free Boron-Mediated -C-H Hydroxylation of -Benzyl-3,4,5-tribromopyrazoles.

A novel route has been reported for C-H hydroxylation of benzyl compounds directed by a 3,4,5-tribromopyrazole auxiliary via boronation/oxidation using BBr and NaBO·4HO. The strategy exhibits outstanding site selectivity and affords the corresponding phenols in moderate to excellent yields under metal-free conditions. Besides, this protocol can be achieved in one pot, which is highly promising as a practical method for use in a multistep organic synthetic process.

Xiaoyaosan ethyl acetate fraction alleviates depression-like behaviors in CUMS mice by promoting hippocampal neurogenesis via modulating the IGF-1Rβ/PI3K/Akt signaling pathway.

Ethnopharmacological Relevance: Xiaoyaosan (XYS), a representative and classic traditional Chinese medicine (TCM) prescription with function of dispersing stagnated liver and strengthening spleen, has been used for thousands of years to treat depression. XYS' anti-depression effect has been demonstrated both clinically and experimentally; however, the material basis for this effect has yet to be elucidated.

Aim Of The Study: This study aimed to evaluate the impact and underlying action mechanism of XYS' antidepressant active component (Xiaoyaosan ethyl acetate fraction, XYSEF) against chronic unpredictable mild stress (CUMS)-induced depression-like behavior in mice.

Ligand-Enabled C-H Olefination and Lactonization of Benzoic Acids and Phenylacetic Acids via Palladium Catalyst.

A novel ligand propan-2-one -(-tolylcarbamoyl) oxime () has been developed to promote C(sp)-H olefination of benzoic acids and phenylacetic acids via a palladium catalyst. With the subsequent lactonization of the olefinated products through 1,4-addition, highly monoselective cyclic lactone products of benzofuranones and benzopyrones were obtained in moderate to excellent yields. The DFT calculation demonstrated that the novel ligand propan-2-one -(-tolylcarbamoyl) oxime () could improve the C-H activation reaction to give cyclic lactone products elegantly.

Rhodium(III)-catalyzed cascade C-H functionalization/annulation of sulfoximines with iodonium ylides for the synthesis of cyclohexanone-1,2-benzothiazines.

A highly efficient Rh(III)-catalyzed cascade C-H activation/annulation of sulfoximines with iodonium ylides under metal-oxidant-free conditions has been reported. The fused cyclohexanone-1,2-benzothiazine scaffold is readily achieved with a one-pot process in this reaction. This protocol exhibits good functional group tolerance and moderate to excellent yields.

Palladium-Catalyzed β-C(sp)-H Arylation of Aliphatic Ketones Enabled by a Transient Directing Group.

The direct arylation of aliphatic ketones has been developed via Pd-catalyzed β-C(sp)-H bond functionalization with 2-(aminooxy)-,-dimethylacetamide as a novel transient directing group (TDG), which showed remarkable directing ability to generate arylated products in moderate to good yields. Furthermore, the reaction can tolerate abundant substrate of ketones and aryl iodides. This study expands the scope of applications for TDGs.

Xiaoyao Pills Ameliorate Depression-like Behaviors and Oxidative Stress Induced by Olfactory Bulbectomy in Rats via the Activation of the PIK3CA-AKT1-NFE2L2/BDNF Signaling Pathway.

Numerous studies have revealed that oxidative stress is closely associated with the occurrence and development of depression. Xiaoyao Pills (XYW) are included in the Chinese Pharmacopoeia and are frequently used for treating anxiety and depression by smoothing the liver, strengthening the spleen, and nourishing the blood. However, the antidepressant effects of XYW have not yet been thoroughly investigated.

Polysaccharides from Laminaria japonica: an insight into the current research on structural features and biological properties.

Laminaria japonica, one of the most widespread seafood consumed in China and many other nations, has been traditionally utilized as an effective therapeutically active substance for treating weight loss, phlegm elimination, and detumescence for more than 2000 years. Numerous studies have found that the polysaccharides play an indispensable role in the nutritional and medicinal value of L. japonica.

Metal-Free -Selective C-H Borylation of 2-Phenylthiopyridines Using BBr.

A novel route for -selective C-H borylation of 2-phenylthiopyridines using BBr as the boron source under metal-free conditions has been reported. The reaction exhibited site exclusivity, and the synthesized aryl boronates were freely converted to various useful intermediates. Thus, this facile method would be beneficial to synthesize structurally diversified phenylthioethers derivatives and other materials containing boron-nitrogen coordination.

Extraction, purification, structural characteristics and biological properties of the polysaccharides from Codonopsis pilosula: A review.

Codonopsis pilosula (Franch.) Nannf., as a well-known homology plant of medicine and food, has the function of replenishing the Qi, strengthening the spleen and tonifying the lung, nourishing the blood and engendering the liquid in traditional Chinese medicine.

Continuous-wave pumped frequency upconversions in an InSe-integrated microfiber.

We report the achievement of continuous-wave (CW)-pumped second-harmonic generation (SHG) and sum frequency generation (SFG) in a layered indium selenide (InSe)-integrated microfiber. As a result of the strong interaction between the InSe nanosheets and the evanescent field, the second-order nonlinear processes are greatly enhanced in the InSe-integrated microfiber pumped by a few milliwatt CW lasers. The experimental results reveal that the intensities of SHG and SFG are quadratic and linear dependencies with the incident pump power, respectively, which is consistent with theoretical predictions.

Maxim.: A Review of Its Traditional Usages, Phytochemical Constituents, and Pharmacological Properties.

Maxim., also known as "Manchurian walnut" (Chinese) and "Onigurumi" (Japanese), is a medicinal plant widely distributed in Western and Central Asia, especially in China. It has been traditionally used to treat cancer, gastric ulcers, diarrhea, dysentery, dermatosis, uterine prolapse, and leukopenia.