A palladium-catalyzed deuterated formylation of aryl sulfonium salts is prepared conveniently from readily available arenes, which enables the expedient synthesis of a series of structurally diverse C-1 deuterated aldehydes with 96%−99% deuterium incorporation. The easy to handle and cost-effective DCOONa provides a deuterium source, which can be introduced onto the formyl units with excellent selectivity under the palladium-catalytic redox neutral conditions. This catalytic route can accomplish the direct late-stage C−H functionalization of bioactive molecules and natural product derivatives assisted by C (sp 2 )−H thianthrenation. Moreover, on the basis of this practical approach, several deuterated drugs and analogues could be prepared with excellent levels of deuterium incorporation.
Allenes and trifluoromethyl motifs are considered as important building blocks in materials and pharmaceuticals. A copper-catalysed synthesis of trifluoromethyl allenes utilizing readily available feedstocks under mild and environmentlly friendly conditions...
Functional molecules bearing polychlorinated moieties usually play versatile roles in organic synthesis and biochemistry. A copper-catalyzed multicomponent polychlorocarboalkynylation of alkenes presents an efficient and operationally simple approach for the synthesis of β-polychlorinated alkynes. Mechanistic experiments were conducted demonstrating that an in situ generated copper acetylide complex was the real catalyst and reactive intermediate during the copper-catalytic cycle. And enantioselective exploration demonstrated potential application for the synthesis of chiral β-polychlorinated alkynes.The Supporting Information is available free of charge at https://pubs.acs.org/doi/10.1021/acs.orglett.2c01755.Detailed experimental procedures, characteristic data, and copies of NMR spectra of compounds. (PDF)
A heterogeneous redox-neutral palladium-catalytic platform was reported for the preparation of deuterated (hetero) arenes from (hetero) arenes mediated by regioselective C(sp2)–H thianthrenation utilizing commercially available and recyclable Pd/C catalyst. A wide range of deuterated compounds could be obtained in high yields with excellent levels of deuterium incorporation under these simple heterogeneous catalytic conditions with the requirement of stable and easily handled DCOONa as a deuterium source. The late-stage deuteration of pharmaceuticals and bioactive molecules was also achieved by this approach.
Backgrounds: Wheat (Triticum aestivum L.) is one of the most important food crops in the world. It faces various abiotic stresses during its growth. Drought is one of the main factors limiting the growth and development of wheat. Severe drought stress will Lead to a decline in wheat production. Cytoplasmic glyceraldehyde-3-phosphate dehydrogenase (GAPC) is an important member of the glyceraldehyde-3-phosphate dehydrogenase (GAPDH) family, which is widely present in plant cytoplasm. Plants play an important role in the process of primary metabolism and stress resistance.Result: In this study, a comparative transcriptomic analysis of the TaGAPCs-RNAi strain of Changwu 134 and the wild-type wheat seedlings of Changwu 134 under natural drought conditions was carried out. A total of 30067 differentially expressed genes were screened in RNAi strains and wild-type strains, of which 19,959 genes were up-regulated in RNAi strains and 10,108 genes were down-regulated in transcription. GO analysis shows that differential genes are mainly enriched in biological regulation, cellular processes, metabolic processes, and responses to stimuli. KEGG analysis showed that the differential genes were mainly concentrated in the biosynthesis of phenylpropane, plant hormone signal transduction and flavonoid biosynthesis pathways. By analyzing the expression levels of differential transcription factors, the significantly down-regulated transcription factor WRKY family member TaWRKY2 / 22/28/29/33/40/47/52 in wheat was screened out. The TaWRKY28/33/40/47 gene silencing line was successfully obtained using the barley stripe mosaic virus (BSMV-VIGS) technology. The plants with TaWRKY28/33/40/47 gene silenced were subjected to natural drought treatment, and physiological and biochemical index tests were carried out. The results showed that the growth status of gene-silenced plants was worse than that of wild-type plants, and the relative water content and chlorophyll content decreased. The content of MDA, H2O2 and superoxide anion increases, the activity of antioxidant enzymes (SOD, POD, CAT) decreases, and the content of proline decreases. Conclusion: The results showed that TaGAPCs regulates the expression of some TaWRKYs transcription factors, activates antioxidant pathways, enhances tolerance of wheat to drought stress.
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