Due to its unique physical and electrophilic properties, the difluoromethyl group (-CF H) has been playing an irreplaceable role in the field of pharmaceutical and agrochemical industry. Methods that could efficiently incorporate the difluoromethyl group into the target molecules are increasing in the recent years. Developing a stable and efficient difluoromethylating reagent is thus highly attractive.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
October 2022
The quest of the active species in copper-mediated difluoromethylation of aryl halides led to the discovery of a powerful difluoromethylating reagent [Ph P] [Cu(CF H) ] 2. Complex 2 was able to difluoromethylate a variety of electrophiles including electron-deficient and electron-rich aryl iodides, heteroaryl iodides, activated heteroaryl bromides, chloride and aryl bromides with a directing group, as well as other electrophiles such as alkenyl iodide, benzyl bromides, allyl bromides, alkyl iodide, allyl carbonates and acid chloride. In addition, in the presence of an oxidant, complex 2 reacted with various lithium nbutyl arylboronic acid pinacol esters, alkyne and heteroarene.
View Article and Find Full Text PDFWe describe, for the first time, two protocols for direct difluoromethylation of unactivated alkyl bromides and iodides. Reactions of alkyl iodides with TMSCFH were mediated by a copper catalyst using CsF as the activator, while reactions of less reactive alkyl bromides required a combination of palladium and a stoichiometric amount of CuI as the catalysts. Preliminary mechanistic studies of the synergistic Pd/Cu-catalyzed difluoromethylation of alkyl bromides suggest that it proceeds likely via a Pd(I)/Pd(III) catalytic cycle.
View Article and Find Full Text PDFBACKGROUND Gastric cancer (GC) remains one of the most fatal digestive cancers in the world; nevertheless, its etiology remains vague. With the development of bioinformatics analysis, numerous circular RNAs (circRNAs) have been found to be dysregulated in GC. However, the functions of a large portion of dysregulated circRNAs in GC need further validation.
View Article and Find Full Text PDFAsian Nurs Res (Korean Soc Nurs Sci)
May 2020
Purpose: Hemiplegic patients often experience malnutrition and feeding risks due to disabilities and inadequate nursing support; nursing roles regarding mealtime assistance remain unclear in China. Therefore, this study aimed to clarify the core knowledge and skills of nursing competency regarding mealtime assistance for hemiplegic patients in China.
Methods: A cross-sectional survey of self-administered questionnaire to 640 nurses (response rate: 57.
A process for the concurrent transfer of both the NHC ligand and the difluoromethyl group from [(SIPr)Ag(CFH)] to PdX (X = Cl, OAc, and OPiv) for the preparation of [(SIPr)Pd(CFH)X] complexes is described. These complexes were air-stable and easily underwent transmetalation with aryl pinacol boronate/reductive elimination to generate ArCFH in high yields. Based on this discovery, the first one-pot C-H borylation and difluoromethylation process for the preparation of difluoromethylated (hetero)arenes was developed.
View Article and Find Full Text PDFIt is well known that existing protected areas (PAs) should function as focal areas for expanding PA systems. The optimal complementary conservation areas are often identified by implementing two approaches in systematic conservation planning, i.e.
View Article and Find Full Text PDFObjective: This study was performed to evaluate the application of enhanced recovery after surgery (ERAS) in patients undergoing radical cystectomy (RC).
Methods: The clinical data of 192 patients who underwent RC were collected in this retrospective cohort study. Among them, 91 patients who underwent ERAS were allocated to the ERAS group, and the remaining 101 patients who underwent traditional postoperative care procedures were allocated to the non-ERAS group.
Prostate cancer antigen 3 (PCA3) is one of the most promising genes currently investigated as a specific tumor biomarker for the diagnosis of prostate cancer. The purpose of this study was to investigate PCA3 gene expression in peripheral blood of prostate cancer (PCa) and benign prostate hyperplasia (BPH), and further to assess its clinical significance. We determined the copies of PCA3 mRNA in peripheral blood of PCa and BPH from 115 samples (PCa, n=78; BPH, n=37) using a quantitative reverse transcriptase-quantitative polymerase chain reaction (RT-qPCR) with TaqMan assay.
View Article and Find Full Text PDFHepatitis C virus (HCV) frequently establishes persistent infections that can develop into severe liver disease. The HCV NS3/4A serine protease is not only essential for viral replication but also cleaves multiple cellular targets that block downstream interferon activation. Therefore, NS3/4A is an ideal target for the development of anti-HCV drugs and inhibitors.
View Article and Find Full Text PDFXi Bao Yu Fen Zi Mian Yi Xue Za Zhi
November 2014
Objective: To establish SMMC-7721 human hepatocellular carcinoma cell line stably expressing hepatitis C virus (HCV) core protein.
Methods: A lentiviral vector containing HCV core gene was constructed and transfected into HEK293T cells to package recombinant lentivirus (rLV-core) containing ZsGreen and HCV core genes. The SMMC-7721 cells were infected with the rLV-core.
rhPTH1-34 is clinically used for osteoporosis treatment. However, this peptide drug has no oral bioavailability because of proteolysis and low membrane permeability in gastrointestinal gut. This study explored the possibility of absorption enhancement for rhPTH1-34 through the oral delivery of the microemulsion.
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