摘要:
Herein, we have revealed elemental sulfur- and iodine reagent-mediated indole C3 arylations using cyclohexanones as the arylating reagent. This protocol provides an efficient gram-scalable access to 3-arylindole and benzo[4,5]thieno[2,3-b]indole motifs with a broad range of compatible functionalities.
摘要:
A three-component procedure for the preparation of 2-substituted benzothiazoles from nitroarenes, alcohols, and sulfur powder is described. The reaction showed a good functional group tolerance to provide the heterocyclic products in moderate to good yields. The sequential assembly involving nitro reduction, C–N condensation, and C–S bond formation has been realized in one pot.
期刊:
NEW JOURNAL OF CHEMISTRY,2019年43(15):6010-6020 ISSN:1144-0546
通讯作者:
Zhou, Wen;Zhou, Li
作者机构:
[Fu, Kaishuo; Yuan, Sisi; Zhou, Wen; Huang, Weiping; Li, MaoLin] Guangzhou Univ Chinese Med, Sch Pharmaceut Sci, Waihuan Rd, Guangzhou 510006, Guangdong, Peoples R China.;[Jiang, Zhilin] Puer Univ, Puer, Yunan, Peoples R China.;[Shi, Yonghui] Sun Yat Sen Univ, Sun Yat Sen Mem Hosp, Dept Pharm, Guangzhou 510120, Guangdong, Peoples R China.;[Chen, YongJun] Guangzhou Univ Chinese Med, South China Res Ctr Acupuncture & Moxibust, Med Coll Acu Moxi & Rehabil, Waihuan Rd, Guangzhou 510006, Guangdong, Peoples R China.;[Zhou, Li] Hunan Agr Univ, Coll Sci, Changsha 410128, Hunan, Peoples R China.
通讯机构:
[Zhou, Wen] G;[Zhou, Li] H;Guangzhou Univ Chinese Med, Sch Pharmaceut Sci, Waihuan Rd, Guangzhou 510006, Guangdong, Peoples R China.;Hunan Agr Univ, Coll Sci, Changsha 410128, Hunan, Peoples R China.
摘要:
The tumor-seeking role of bleomycin (BLM) disaccharide has been demonstrated to serve as a promising tool for cancer diagnosis and a potential ligand for targeted therapy. However, these practical applications are often hampered by the lack of BLM disaccharide. Herein, an efficient multi-gram synthesis of peracetylated BLM disaccharide 20 is achieved by a TMSOTF-mediated glycosidation coupling manner in 43.6% overall yield in terms of benzyl galactoside. The critical innovation of the synthetic strategy is that inexpensive benzyl galactoside was first adopted to prepare an l-gulose subunit 3 as a glycosyl acceptor, with a much shorter route in 73.0% yield, and a 3-O-carbamoyl-mannose donor 4 was achieved in 47.2% yield by lowering the amount of dibutyltin oxide, and merging aminolysis and selective deacetylation into a one-pot reaction. Next, the incorporation of BLM disaccharide into 10-hydroxycamptothecin (10-HCPT), a non-specific model compound, to form conjugate 1 could significantly improve the antitumor activity and display obvious selectivity toward cancerous and normal cells in comparison with 10-HCPT. Moreover, BLM disaccharide itself was non-cytotoxic, clearly indicating the importance and potential of BLM disaccharide in solving the targeted antitumor therapy of cytotoxic drugs.
通讯机构:
[Huang, Huawen] X;Xiangtan Univ, Coll Chem, Key Lab Green Organ Synth & Applicat Hunan Prov, Minist Educ,Key Lab Environm Friendly Chem & Appl, Xiangtan 411105, Peoples R China.
摘要:
A novel copper-catalyzed oxidative formal [3 + 2] annulations of ketoxime acetates and tetrohydroisoquinolines for the synthesis of fused pyrazoles and imidazoles has been developed. A broad range of important isoquinoline-fused pyrazole and imidazole products were selectively generated by the key control of oxidant.
摘要:
A DNA-templated copper nanoparticle (CuNP) probe has been developed for the determination of the human immunodeficiency virus oligonucleotide (HIV-DNA). The function of the probe relies on affinity binding-induced DNA hybridization associated with the use of double G-quadruplexes. Double-stranded DNA (dsDNA) with poly(AT-TA) bases was used as a template for synthesis of dsDNA-CuNPs. These have weak fluorescence. In the next step, two G-rich sequences that are linked to both sides of the ds-DNA are locked by HIV complementary DNA (cDNA). If HIV-DNA is introduced, it will hybridize with cDNA, thereby transforming the two G-rich sequences into G-quadruplexes. This enhances the fluorescence of the adjacent dsDNA-CuNPs. Fluorescence increases linearly in the 1 to 200 and 250-1000 nM HIV-DNA concentration range, and the detection limit is 13 pM. This enzyme-free fluorometric assay is time-saving, easily operated, and therefore has large potential in biosensing because it may be extended to various other DNA targets. Graphic abstract Double-strand DNA-templated copper nanoparticles (DNA-CuNPs) have weak fluorescence. When Human Immunodeficiency Virus oligonucleotide (HIV-DNA) is added, it completely hybridized with HIV complementary DNA (cDNA). As a result, the two exposed G-rich sequences are transformed into G-quadruplexes, and an apparent increase in the fluorescence intensity can be observed. (AA: ascorbic acid).
摘要:
Regioselective azotization or bis(amination) products of the title porphyrinoid were achieved in one-pot one-step syntheses under mild conditions using a selection of aromatic amines and isoamyl nitrite or p-chloranil, respectively. Structures, tautomery, chirality as well as spectroscopic and redox properties of the new systems were discussed.
摘要:
We present an atomistic simulation study on the compositional arrangements throughout Cu-Pt icosahedra, with a specific focus on the effects of inherent strain on general segregation trends. The coexistence of radial and site-selective segregation patterns is found in bimetallic nanoparticles for a broad range of sizes and compositions, consistent with prior analytical and atomistic models. Through a thorough comparison between the composition patterns and strain-related patterns, it is suggested that the presence of gradient and site-selective segregation is natural to largely relieve the inherent strain by preferential segregation of big atoms at tensile sites and vice versa, as previously hypothesized in the literature. Analogous to the case of single crystal particles, Cu-rich surface and damped oscillations can also be found in the outer shells of icosahedra, which are dominated by the lowering of both the surface energy and the chemical energy. The thermodynamic stability of segregated icosahedra is similar to segregated cuboctahedra but higher than disordered bulk alloys, validating prior thinking that element segregation driven by strain relief can extend the stability range of multiply-twinned nanoparticles. Our work sheds new light on understanding strain-induced segregation in multiply-twinned nanosystems that have elements with large lattice mismatch and strong alloying ability.
通讯机构:
[Zhang, Feng] H;[Gong, Hang] X;Hunan Agr Univ, Coll Sci, Changsha 410128, Hunan, Peoples R China.;Xiangtan Univ, Coll Chem, Key Lab Environmentally Friendly Chem & Applicat, Key Lab Green Organ Synth & Applicat Hunan Prov, Xiangtan 411105, Peoples R China.
摘要:
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 degrees 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.
关键词:
Lithium ion batteries;Li-rich layered material;Hollow-microspheres;High capacity
摘要:
Li-rich layered Li2MnO3 is of great attraction for high energy lithium ion batteries. However, its cycling is still needed for improvements. Here we report a hollow microsphere-structured xLi(2)MnO(3)center dot(1-x)LiNiO2 (x = 0.3-0.7) that is synthesized by using in-situ template-sacrificial strategy. Powder X-ray diffraction (XRD) and scanning electron microscope (SEM) characterizations prove that thexLi(2)MnO(3)center dot(1-x)LiNiO2 (x = 0.3-0.7) are based on monoclinic Li2MnO3 with alpha-NaFeO2 layered structure in which Li+ ions are orderly arranged in the transition metal layers, and the hollow-microspheres have diameters of similar to 3 mu m. Electrochemical results show that the optimal ratio of Li2MnO3/LiNiO(2 )is 0.6/0.4. As a consequence, the stabilized discharge capacity of 0.6Li(2)MnO(3)center dot 0.4LiNiO(2) (0.6LLMNO) is similar to 210 mAh g(-1) after the first few cycles. This shows that appropriate amount Ni substitution for Mn in Li2MnO3 helps to improve the specific capacity and cycling stability. (C) 2019 Elsevier B.V. All rights reserved.
通讯机构:
[Cai, Changqun] X;Xiangtan Univ, Key Lab Green Organ Synth & Applicat Hunan Prov, Key Lab Environm Friendly Chem & Applicat, Minist Educ,Coll Chem, Xiangtan 411105, Peoples R China.
关键词:
Ag nanoclusters;Simultaneous detection;HIV DNA;Label-free
摘要:
A novel DNA-stabilized silver nanoclusters (AgNCs)-based label-free fluorescent platform for simultaneously detecting two human immunodeficiency virus oligonucleotides (HIV DNAs) was developed. The sensing platform was established based on fluorescence enhancement of guanine (G)-rich and the phenomenon in the process of two silver nanoclusters (AgNCs) forming a nanoclusters dimer. The probe (AgNCs/G) utilized for HIV-1 detection adopted an effective conformation based on enhancement effect of G-rich sequence (at 500 nm ex / 565 nm em) while the probe (AgNCs/AgNCs) for HIV-2 generated fluorescence signals (at 580 nm ex / 630 nm em) with bright fluorescence only in nanoclusters dimer. The nanoprobe shows high selectivity for multiplexed analysis of target DNA with a detection limit of 11 pM, respectively. Moreover, this is the first time to use the affectivity of fluorescent AgNCs and two HIV DNAs simultaneous detection integrated into a novel method, which shows a great promise in biomedical research and early clinical diagnosis.
摘要:
The enhancement of surface functional groups of biochar is essential to improving the biochar contaminant adsorption. Current pyrolysis methods that are accompanied by activation are energy consuming and costly. Herein, a novel wet-pyrolysis system that was carried out in open air, with simultaneous conversion and modification to produce an effective biochar adsorbent, is described. Within this system, the surface of the biochar was oxidized partially to produce sufficient functional groups at the surface, whereas carbonization of thebiomass (miscanthus sacchariflora) occurs under an acidic catalyst. The characteristic results confirmed the attachment of abundant surface functional groups, including hydroxyl and carboxyl groups, which increased in content with the ongoing reaction time. Neutralization with sodium carbonate removed the hydrogen bonds and enhanced the adsorption properties. The biochar that was obtained by using this technique exhibited an excellent cadmium adsorption capacity of 197 mg.g(-1) and a high removal efficiency of 99%. Analysis of the Cd-loaded biochar indicated that adsorption occurred via ion exchange, and formed cadmium complexes. It could be concluded that this novel wet-pyrolysis system is a promising approach to produce biochar efficiently and cost-effectively for heavy-metal remediation. (C) 2019 Elsevier Ltd. All rights reserved.
摘要:
A simple, practical and metal-free method has been developed for the synthesis of sulfonamides and β-arylsulfonyl enamines via the selective cleavage of C–N and C–H bonds through the iodine-catalyzed oxidation of arenesulfonyl chlorides and sodium sulfinates with tert-amines. The method uses commercially available inexpensive catalysts and oxidants, and has a wide substrate scope and operational simplicity.
期刊:
JOURNAL OF THE ELECTROCHEMICAL SOCIETY,2019年166(15):B1491-B1496 ISSN:0013-4651
通讯作者:
Peng, Chang;Zhao, Peng
作者机构:
[Liu, Xiaoying; Zhang, Silu; Peng, Chang; Zhou, Bijing; Li, Wenbin; Li, Muyi; Zeng, Tianqin] Hunan Agr Univ, Coll Sci, Changsha 410128, Hunan, Peoples R China.;[Zhao, Peng] Southern Med Univ, Sch Pharmaceut Sci, Guangdong Prov Key Lab New Drug Screening, Guangzhou Key Lab Drug Res Emerging Virus Prevent, Guangzhou 510515, Guangdong, Peoples R China.
通讯机构:
[Peng, Chang] H;[Zhao, Peng] S;Hunan Agr Univ, Coll Sci, Changsha 410128, Hunan, Peoples R China.;Southern Med Univ, Sch Pharmaceut Sci, Guangdong Prov Key Lab New Drug Screening, Guangzhou Key Lab Drug Res Emerging Virus Prevent, Guangzhou 510515, Guangdong, Peoples R China.
摘要:
Heteroatom doped carbon materials have attracted intense attention in constructing electrochemical sensors because of their outstanding electrocatalytic performance. Up to now, most of the researches were focused on the electrochemical application of single heteroatom doped carbon microspheres. In this work, N, P-co-doped carbon microspheres (NP-CMs) modified electrode was developed as highly sensitive electrochemical sensor for acetaminophen. NP-CMs were acquired by the calcination of products from the one-pot reaction of dopamine and 9,10-dihydro-9-oxa-10-phosphaphenanthrene-10-oxide (DOPO). Experimental results revealed that NP-CMs showed better electrocatalytic performance compared with N-doped carbon microspheres. Under the optimal conditions, the response of NP-CMs/GCE showed a linear relationship with acetaminophen concentration from 0.07 mu M to 30 mu M, the linear equation was Y = 0.01356X+0.7417 and the detection limit was 40 nM (S/N = 3). The recoveries of the NP-CMs modified GCE for the assay of acetaminophen in human serum samples were from 94.0% to 106.0%. It was believed that N, P-co-doped carbon microspheres have a great potential in the design of novel pharmaceutical analysis methods. (C) 2019 The Electrochemical Society.