Synthesis of Pyrimido[1,2-a]indolediones and Pyrimidinediones via [4+2] Annulation of 2H-Azirine-2-carbaldehydes.

NHC-catalyzed [4+2] annulation of 2H-azirine-2-carbaldehydes with ketimines and isocyanates has been developed, providing straightforward synthetic protocols for constructing structurally intriguing pyrimido[1,2-a]indolediones and pyrimidinediones under mild conditions with excellent yields. This protocol can be used to synthesize the core skeleton of pharmaceutically important drugs and pyrimido[1,2-a]indoledione-containing natural products, making it potentially valuable for creating biologically active derivatives.

Control of Aluminum and Titanium Contents in the Electroslag Remelting of ATI 718PlusTM Alloy.

The burning loss of Al and Ti elements in superalloys during electroslag remelting has become a prevalent issue. And the existing slag system is not suitable for smelting the ATI 718PlusTM alloy. Therefore, it is imperative to develop a new slag system for smelting the ATI 718PlusTM alloy. To mitigate this issue, a thermodynamic model of the oxidation reaction of Al and Ti at the slag and alloy interface was established based on the ion and molecule coexistence theory (IMCT). The thermodynamic model was used to investigate the correlation between the equilibrium content of Al and Ti, slag composition, smelting temperature, and initial Al and Ti content of the electrode. The results indicate that while increasing the smelting temperature can effectively inhibit the burning loss of Al, it will exacerbate the burning loss of Ti. Increasing CaO and Al2O3 contents can inhibit the Al burning loss, while an increase in the TiO2 content can inhibit the Ti burning loss. Although an increase in the MgO content results in the burning loss of Al, its impact on the Al is minimal. The burning loss of Al and Ti was not affected by the change in the CaF2 content. The high Al content in ATI 718PlusTM makes it prone to burning loss of Al during the electroslag remelting. The combustion loss of Al can be reduced by increasing the Ti content in the electrode or adding a suitable amount of aluminum powder to the slag system. The accuracy of the model had been validated through experimental verification.

Catalytic Asymmetric Synthesis of 3,4'-Piperidinoyl Spirooxindoles via [3 + 3] Annulation of 3-Aminobenzofurans and Isatin-Derived Enals.

A chiral NHC-catalyzed [3 + 3] cycloaddition reaction of 3-aminobenzofurans with isatin-derived enals has been documented, furnishing 3,4'-piperidinoyl spirooxindoles bearing a quaternary stereocenter with good yields and excellent enantioselectivities. Further gram-scale preparation and synthetic transformation of the cycloadducts to δ-amino acid derivative demonstrated good practicality and applicability of this reaction.

Synthesis of Pyridazino[4,5-b]indoles by [3+3] Annulation of 2-Alkenylindoles and Hydrazonyl Chlorides.

A novel [3+3] annulation reaction of 2-alkenylindoles with hydrazonyl chlorides in the presence of base for the formation of pyridazino[4,5-b]indoles was developed. This approach provided a convenient and efficient way to synthesize a series of functionalized pyridazino[4,5-b]indoles derivatives. The method exhibited a broad substrate scope and provided the corresponding pyridazino[4,5-b]indoles products with excellent yields.

Prevalence and Genotype of Trichomonas vaginalis among Men in Xinxiang City, Henan Province, China.

Trichomonas vaginalis (T. vaginalis) could cause trichomoniasis through sexual transmission, which was globally distributed. In this study, the prevalence and phylogenetic analyses of T. vaginalis among men in Xinxiang were conducted. From October 2018 to December 2019, a total of 634 male clinical samples were collected, including 254 samples of semen, 43 samples of prostate fluid, and 337 samples of urine. These samples were examined by nested PCR and a total of 32 (5.05%) T. vaginalis-positive samples were detected. Among these samples, the positive rates of T. vaginalis in semen, prostate fluid, and urine were 7.87% (20/254), 4.65% (2/43), and 2.97% (10/337), respectively. Three actin genes were successfully isolated and sequenced from the 32 positive DNA samples, and the analysis of the sequence and phylogenetic tree showed that the three actin gene sequences exhibited 99.7%-100% homology to the published actin gene sequence (EU076580) in NCBI, and the T. vaginalis strains in the three positive samples were identified as genotype E. Our results demonstrate a notable genotype of T. vaginalis in the male population and provide insight into the performance of these genetic markers in the molecular epidemiology of trichomoniasis. However, further studies are needed to research the association between the genotype and the pathogenicity of T. vaginalis.

Iron-Catalyzed Cleavage Reaction of Keto Acids with Aliphatic Aldehydes for the Synthesis of Ketones and Ketone Esters.

The radical-radical coupling reaction is an important synthetic strategy. In this study, the iron-catalyzed radical-radical cross-coupling reaction based on the decarboxylation of keto acids and decarbonylation of aliphatic aldehydes to obtain valuable aryl ketones is reported for the first time. Remarkably, when tertiary aldehydes were used as carbonyl sources, ketone esters were selectively obtained instead of ketones. The gram-scale preparation of aryl ketone through this strategy was easily achieved by using only 3 mol % of the iron catalyst. As a proof-of-concept, the bioactive molecule flurprimidol was synthesized in two steps by using this strategy.

MoS2-Catalyzed transamidation reaction.

The MoS2-catalyzed transamidation reaction with high yields using N,N-dimethylformamide and other amides as carbonyl sources is developed here. The protocol is simple, does not require any additive such as acid, base, ligand, etc., and encompasses a broad substrate scope for primary, secondary and heterocyclic amines. Moreover, the acetylation and propanylation of amines also can be achieved with good to excellent yield by this strategy.

Metal- and solvent-free synthesis of amides using substitute formamides as an amino source under mild conditions.

This study described an efficient and practical approach for amide synthesis. The reaction was conducted under metal- and solvent-free conditions at a mild temperature (40 °C) in air, and readily available formamides were used as an amino source. This reaction can be easily upgraded to the gram level with an excellent yield.

Palladium-Catalyzed Direct α-Ketoesterification of 8-Methylquinoline Derivatives with α-Ketoacids via Dehydrogenation Coupling Reaction.

A direct, regiospecific, and efficient palladium-catalyzed α-ketoesterification of 8-methylquinoline derivatives to generate α-ketoesters has been discovered. This reaction is conducted at a mild temperature, free of peroxide, and compatible with air, and various α-ketoesters were achieved with good yields. Importantly, this reaction can be easily amplified to gram level using only 1 mol % of the palladium catalyst, indicating that there is the potential for further reduction of the amount of catalyst loading required for large-scale production.

Tandem Oxidative Ring-Opening/Cyclization Reaction in Seconds in Open Atmosphere for the Synthesis of 1-Tetralones in Water-Acetonitrile.

A mild and practical tandem oxidative ring-opening/cyclization reaction mediated by Ce4+ for the synthesis of 1-tetralones is presented. This rapid transformation was completed within 30 s and conducted in an open reactor at 0 °C in a water-acetonitrile mixture. Various cyclobutanol derivatives are transformed into desired products in good to high yields, and this reaction can be easily scaled up to the gram scale.