- Acetylcholinesterase-induced fluorescence turn-off of an oligothiophene-grafted quartz surface sensitive to myristoylcholine
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Conjugated polyelectrolytes (CPEs) have recently emerged as label-free materials for biosensing due to their intrinsic ability to transduce an amplified optical signal in response to interactions with different analytes. Herein, the conformational change of an anionic oligothiophene is exploited to generate a unique fluorescent response upon interaction with myristoylcholine (MyrCh). The variations observed in spectroscopic signals are explained in terms of a synergistic combination of hydrophobic and electrostatic forces involving the oligothiophene chains and MyrCh molecules, inducing the disassembling of oligothiophene chains. The enzyme acetylcholinesterase (AChE) is able to reverse this effect by catalyzing the hydrolysis of MyrCh; hence, its enzymatic activity can be monitored through the variation of fluorescence emission of the system. The oligothiophene sensing probe retains its conformational sensitivity with regard to the AChE-mediated cleavage of MyrCh upon immobilization onto a quartz substrate, which is accomplished by a "grafting onto" approach based on click chemistry. These results are encouraging for the further development of such a label-free system towards the fabrication of sensing devices that would incorporate CPEs and would be potentially useful for the specific detection of a wide range of bioanalytes. This journal is
- Grisci,Mróz,Giovanella,Pagano,Porzio,Ragona,Samperi,Tomaselli,Galeotti,Destri
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- Enantio- and Diastereoselective, Complete Hydrogenation of Benzofurans by Cascade Catalysis
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We report an enantio- and diastereoselective, complete hydrogenation of multiply substituted benzofurans in a one-pot cascade catalysis. The developed protocol facilitates the controlled installation of up to six new defined stereocenters and produces architecturally complex octahydrobenzofurans, prevalent in many bioactive molecules. A unique match of a chiral homogeneous ruthenium-N-heterocyclic carbene complex and an in situ activated rhodium catalyst from a complex precursor act in sequence to enable the presented process.
- Gallagher, Timothy,Glorius, Frank,Hu, Tianjiao,Moock, Daniel,Wagener, Tobias
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supporting information
p. 13677 - 13681
(2021/05/10)
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- Synthesis of sorafenib analogues incorporating a 1,2,3-triazole ring and cytotoxicity towards hepatocellular carcinoma cell lines
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A series of 1,2,3-triazole-containing Sorafenib analogues, in which the aryl urea moiety of Sorafenib (1) was replaced with a 1,2,3-triazole ring linking a substituted phenoxy fragment, were prepared successfully via Huisgen 1,3-dipolar cycloaddition and
- Palakhachane, Sarinya,Ketkaew, Yuwaporn,Chuaypen, Natthaya,Sirirak, Jitnapa,Boonsombat, Jutatip,Ruchirawat, Somsak,Tangkijvanich, Pisit,Suksamrarn, Apichart,Limpachayaporn, Panupun
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- FUSED PYRIMIDINE COMPOUNDS AS KCC2
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The invention concerns compounds of Formula (I): (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and ring A have any of the meanings hereinbefore defined in the description; process for their preparation; pharmaceutical compositions containing them and their use in treating KCC2 mediated diseases.
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Page/Page column 40; 47
(2021/09/17)
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- Enantioselective Palladium-Catalyzed Hydrophosphinylation of Allenes with Phosphine Oxides: Access to Chiral Allylic Phosphine Oxides
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A Pd-catalyzed hydrophosphinylation of alkyl and aryl-oxyallenes with phosphine oxides has been developed for the efficient and rapid construction of a family of chiral allylic phosphine oxides with a diverse range of functional groups. This methodology was further applied in the facile construction of chiral 2H-chromene and later stage functionalization of cholesterol.
- Wang, Jun,Yang, Zhiping
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supporting information
p. 27288 - 27292
(2021/11/17)
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- Enantioselective Synthesis of 3-Fluorochromanes via Iodine(I)/Iodine(III) Catalysis
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The chromane nucleus is common to a plenum of bioactive small molecules where it is frequently oxidized at position 3. Motivated by the importance of this position in conferring efficacy, and the prominence of bioisosterism in drug discovery, an iodine(I)/iodine(III) catalysis strategy to access enantioenriched 3-fluorochromanes is disclosed (up to 7:93 e.r.). In situ generation of ArIF2 enables the direct fluorocyclization of allyl phenyl ethers to generate novel scaffolds that manifest the stereoelectronic gauche effect. Mechanistic interrogation using deuterated probes confirms a stereospecific process consistent with a type IIinv pathway.
- Daniliuc, Constantin G.,Gilmour, Ryan,Neufeld, Jessica,Sarie, Jér?me C.,Thiehoff, Christian
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supporting information
p. 15069 - 15075
(2020/06/17)
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- Synthesis, characterization, and antiplasmodial efficacy of sulfonamide-appended [1,2,3]-triazoles
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A series of benzenesulfonamide-appended [1,2,3]-triazole hybrids was synthesized by using [3 + 2] cycloaddition of primary, secondary, and tertiary sulfonamide azides with various phenoxymethylacetylenes under click reaction conditions. After structural c
- Batra, Neha,Dutta, Roshan Kumar,Ghosh, Prahlad C.,Gupta, Rinkoo D.,Lathwal, Ankit,Nath, Mahendra,Rajendran, Vinoth,Wadi, Ishan
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- TiO2/Cu2O nanoparticle-catalyzed direct C(sp)-P bond formation: Via aerobic oxidative coupling in air and visible light
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The synthesis of organophosphorus compounds is one of the important goals in organic chemistry. Among these compounds, alkynylphosphonates are significantly utilized as the main precursors for the synthesis of biologically active molecules in medicinal chemistry and have attracted extensive interest in the past few decades. Although few efforts have been made towards the direct and atom-economical synthesis of alkynylphosphonates, efforts towards the utilization of visible light as a green and renewable energy source have not been made to date. Here, we have promoted a strategy to construct a type of nano metal oxide composite photocatalyst (Cu2O decorated on TiO2) for the synthesis of alkynylphosphonates via direct C-P bond formation between terminal alkyne and H-phosphonate under visible light irradiation. In this p-n heterojunction photocatalyst, Cu2O acted as a visible-light absorber; moreover, the CB (conduction band) of TiO2 was favorable for accepting a photogenerated electron, and the generated electron hole (e-/h+) pair could initiate the reaction. The present study can provide a new way for the synthesis of this important class of phosphorus organic compounds.
- Hosseini-Sarvari, Mona,Jafari, Fattaneh
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supporting information
p. 3001 - 3006
(2020/03/13)
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- 1,2,3-Triazole-based kojic acid analogs as potent tyrosinase inhibitors: Design, synthesis and biological evaluation
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A series of kojic acid-derived compounds 6a-p bearing aryloxymethyl-1H-1,2,3-triazol-1-yl moiety were designed by modifying primary alcoholic group of kojic acid as tyrosinase inhibitors. The target compounds 6a-p were synthesized via click reaction. All
- Ashooriha, Morteza,Khoshneviszadeh, Mehdi,Khoshneviszadeh, Mahsima,Moradi, Seyed Ershad,Rafiei, Alireza,Kardan, Mostafa,Emami, Saeed
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p. 414 - 422
(2018/11/21)
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- New phenoxymethyl substituted mesoionic triazolium salts: Synthesis and structural characterisation
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A new set of mesoionic 1,2,3-triazolium salts functionalised by para substituted phenoxymethyl side groups were prepared using the ‘click’ Cu catalyzed [3 + 2] cycloaddition of organic azides and terminal alkynes. Four previously unreported neutral triazoles (1–4) were first isolated en route to formation of the salts (5–8). All the compounds were fully characterised (1H, 13C NMR; IR; HR-MS; EA) and representative neutral triazoles and salts were structurally characterised by single crystal X-ray diffraction (SCXRD). Full examination of structural characteristics of the neutral compounds and the salts were presented by detailed analysis of multinuclear NMR data and SCXRD. As metal-free catalysts for the transfer hydrogenation of ketones to alcohols in isopropanol as solvent and hydrogen source, salts 5–8 showed moderate activities for the transformation of acetophenone to 1-phenyl alcohol.
- Dhimba, George,Lawal, Nasir S.,Bala, Muhammad D.
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p. 100 - 107
(2018/11/30)
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- Preparation of novel 1,2,3-triazole furocoumarin derivatives via click chemistry and their anti-vitiligo activity
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The extracts of Psoralea corylifolia?L. were often used for the repigmentation of leukoderma (vitiligo) in traditional Uygur medicine thousands years ago. Nowadays, its active ingredient, furocoumarins, has been clinically applied since it exhibited stron
- Niu, Chao,Lu, Xueying,Aisa, Haji Akber
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p. 1671 - 1678
(2019/01/24)
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- Discovery of a novel series of hDHODH inhibitors with anti-pulmonary fibrotic activities
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Human dihydroorotate dehydrogenase (hDHODH) is a flavin-dependent enzyme essential to pyrimidine de novo biosynthesis, which serves as an attractive therapeutic target for the treatment of autoimmune disorders. A novel series of hDHODH inhibitors was deve
- Lu, Kuan,Zhao, Yanfang,Wu, Guodong,Hu, Hao,Wang, Mingzhong,Gong, Guowei,Jiang, Yuyang
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- Synthesis of 3-Organoselenyl-2H-Coumarins from Propargylic Aryl Ethers via Oxidative Radical Cyclization
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A metal-free oxidative radical cyclization/selenylation of propargylic aryl ethers with diaryl diselenides was developed. This protocol provided an alternative method to synthesize 3-organoselenyl-2H-coumarins via the formation of C?Se bond, C?C bond, and C=O bond in one step. Moreover, a broad range of functional groups (such as halogen, aldehyde, ketone, cyano, and nitro group) were tolerated. (Figure presented.).
- Fang, Jun-Dan,Yan, Xiao-Biao,Zhou, Li,Wang, Yu-Zhao,Liu, Xue-Yuan
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supporting information
p. 1985 - 1990
(2019/03/13)
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- Gold(III)-Catalyzed Intermolecular Oxidation-Cyclization of Ynones: Access to 4-Substituted Chroman-3-ones
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A synthesis of 4-substituted chroman-3-one derivatives has been developed through a gold(III) catalyzed oxidation-cyclization of ynones in good to excellent yield using easily prepared substrates. A broad range of synthetically useful functional groups (halide, alkene, alkyne, phenolic hydroxyl) were tolerated. Further application of this method paves a new way to prepare the skeleton of oblarotenoids. A cascade oxidative cyclization for construction of pyrano[2,3-c]chromen-1(5H)-one derivatives is also presented. (Figure presented.).
- Li, Jian,Yang, Fang,Ma, Yang-Ting,Ji, Kegong
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supporting information
p. 2148 - 2153
(2019/03/28)
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- Novel triazole-tetrahydroisoquinoline hybrids as human aromatase inhibitors
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Novel thirteen triazole-tetrahydroisoquinoline derivatives (2a-m) were synthesized and evaluated for their aromatase inhibitory activities. Seven triazoles showed significant aromatase inhibitory activity (IC50 = 0.07–1.9 μM). Interestingly, th
- Chamduang, Chanamon,Pingaew, Ratchanok,Prachayasittikul, Veda,Prachayasittikul, Supaluk,Ruchirawat, Somsak,Prachayasittikul, Virapong
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- Copper(II) schiff base complexes with catalyst property: Experimental, theoretical, thermodynamic and biological studies
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Two novel copper(II) Schiff base complexes were synthesized and characterized by various physico-chemical and spectroscopic methods, revealing a distorted square planar geometry around the copper atom. The analytical data confirmed the 1:1 metal to ligand
- Esmaielzadeh, Sheida,Zarenezhad, Elham
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p. 416 - 428
(2018/07/05)
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- Synthesis of Tetrasubstituted α,β-Unsaturated Aldehydes via Radical 1,4-Aryl Migration/Trifluoromethylthiolation Cascade Reaction of Aryl Propynyl Ethers
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A one-pot synthesis of tetrasubstituted acrylaldehydes via difunctionalization of aryl propynyl ethers has been achieved, which involves a trifluoromethylthiolation process and a radical 1,4-aryl migration from oxygen to carbon. The reaction shows excellent conversion of aryl propynyl ethers into trifluoromethyl-containing α,β-unsaturated aldehydes through a radical pathway. (Figure presented.).
- Guo, Chun-Huan,Chen, Dao-Qian,Chen, Si,Liu, Xue-Yuan
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supporting information
p. 2901 - 2906
(2017/09/08)
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- Design and synthesis of 1,2,3-triazole-etodolac hybrids as potent anticancer molecules
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A series of novel 1,2,3-triazole-etodolac hybrids (6a-l) were designed and synthesized as potent anti-cancer molecules. The synthesis strongly relied on Huisgen's 1,3-dipolar cycloaddition between etodolac azide 3 and substituted terminal alkynes 5a-l. Th
- Kummari, Bhaskar,Polkam, Naveen,Ramesh, Perla,Anantaraju, Hasithashilpa,Yogeeswari, Perumal,Anireddy, Jaya Shree,Guggilapu, Sravanthi Devi,Babu, Bathini Nagendra
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p. 23680 - 23686
(2017/07/07)
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- Efficient synthesis of new antiproliferative steroidal hybrids using the molecular hybridization approach
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A series of steroidal hybrids with different terminal bioactive scaffolds were synthesized using the molecular hybridization approach and further evaluated for their antiproliferative activity against several cancer cell lines of different origins using t
- Yu, Bin,Qi, Ping-Ping,Shi, Xiao-Jing,Huang, Ruilei,Guo, Hao,Zheng, Yi-Chao,Yu, De-Quan,Liu, Hong-Min
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p. 241 - 255
(2016/04/26)
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- Synthesis and antibacterial evaluation of novel sulfonamide based [1,2,3]-triazoles
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A new series of sulfonamide based [1,2,3]-triazoles 4a-i, 5 and 6 has been prepared in 65-99% yield through Huisgen [3+2] cycloaddition reaction of 4-azido-N-substitutedbenzenesulfonamides 2a,b with various alkynes (3a-i or phenyl acetylene) in the presence of CuSO4.5H2O and sodium ascorbate in t-butanol and water (1:1) mixture at 40°C. The structures of all the newly synthesized molecules have been established on the basis of IR, 1H and 13C NMR and high resolution mass spectral analysis. Furthermore, these compounds have been evaluated for their preliminary in vitro antibacterial activity against two Gram-negative bacteria viz. Escherichia coli (MTCC 433) and Salmonella enterica ser. typhi (MTCC 733) and a Gram-positive bacterium viz. Streptococcus mutans (MTCC 497) by using MTT assay.
- Batra, Neha,Roy, Basabi,Mazumder, Sibnath,Nath, Mahendra
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p. 650 - 655
(2015/05/27)
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- Gold(I)-Catalyzed Dearomative [2+2]-Cycloaddition of Indoles with Activated Allenes: A Combined Experimental-Computational Study
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The gold-catalyzed synthesis of methylidene 2,3-cyclobutane-indoles is documented through a combined experimental/computational investigation. Besides optimizing the racemic synthesis of the tricyclic indole compounds, the enantioselective variant is pres
- Ocello, Riccardo,De Nisi, Assunta,Jia, Minqiang,Yang, Qing-Qing,Monari, Magda,Giacinto, Pietro,Bottoni, Andrea,Miscione, Gian Pietro,Bandini, Marco
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supporting information
p. 18445 - 18453
(2015/12/24)
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- Synthesis of Potential Bioactive Novel 7-[2-Hydroxy-3-(1,2,3-triazol-1-yl) propyloxy]-3-alkyl-4-methylcoumarins
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A series of 50 novel 7-[2-hydroxy-3-(1,2,3-triazol-1-yl)propyloxy]-3-alkyl-4-methylcoumarins had been designed and synthesized in good to excellent yields via Cu(I)-catalyzed 1,3-dipolar cycloaddition reaction "click chemistry" of 7-(3-azido-2-hydroxypropyloxy)-3-alkyl-4-methylcoumarins with variety of acetylene derivatives. In turn, the precursor compound, that is, 7-(3-azido-2-hydroxypropyloxy)-3-alkyl-4-methylcoumarin, was synthesized by condensation of epichlorohydrin with 7-hydroxy-3-alkyl-4-methylcoumarins followed by opening of the epoxide ring in the resulted 7-epoxymethoxy-3-alkyl-4-methylcoumarins with sodium azide. All the synthesized compounds were unambiguously identified on the basis of their spectral data analyses (IR, 1H-NMR, 13C-NMR spectra, and HRMS).
- Arya, Anu,Kumar, Vinod,Mathur, Divya,Singh, Sukhdev,Brahma, Raju,Singh, Rajpal,Singh, Seema,Sharma,Parmar, Virinder S.,Prasad, Ashok K.
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- Cu(I)-catalyzed efficient synthesis of 2'-triazolo-nucleoside conjugates
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A small library of thirty-two 2'-triazolyl uridine and 2'-triazolyl-5-methyluridine has been synthesized by Cu(I)-catalyzed condensation of 2'-azido-2'-deoxyuridine and 2'-azido-2'-deoxy-5-methyluridine with different alkynes and aryl propargyl ethers in almost quantitative yields. Triazolo-nucleoside conjugates, which can be evaluated for different biological activity for suitable drug development, were unambiguously identified on the basis of 1H NMR, 13C NMR, IR, and HRMS data analysis. These compounds have been synthesized for the first time and have not been reported in the literature earlier.
- Mathur,Rana,Olsen,Parmar,Prasad
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p. 701 - 710
(2015/05/13)
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- 'Click' ligand for 'click' chemistry: (1-(4-methoxybenzyl)-1-H-1,2,3-triazol-4-yl)methanol (MBHTM) accelerated copper-catalyzed [3+2] azide-alkyne cycloaddition (CuAAC) at low catalyst loading
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Readily accessible, cost effective, remarkably stable and easily tunable 1,2,3-triazole based ligand, (1-(4-methoxybenzyl)-1-H-1,2,3-triazol-4-yl)methanol (MBHTM) synthesized itself by 'click' chemistry shown to promote the dramatic rate enhancement of co
- Tale, Rajesh H.,Gopula, Venkatesh B.,Toradmal, Gopal K.
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supporting information
p. 5864 - 5869
(2015/11/02)
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- A click chemistry approach for the synthesis of mono and bis aryloxy linked coumarinyl triazoles as anti-tubercular agents
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A series of mono and bis-triazole coumarin hybrids 6aeu and 9aef respectively have been synthesized using 4-(azidomethyl)-2H-chromen-2-ones 5aei and aryl propargyl ethers 2aec/8 employing Click chemistry modified protocol for Azide-Alkyne cycloadditions(CuAAC). Anti-tubercular screening showed moderate activity for mono aryloxy compounds 6aeu with MIC 50-100 μg/mL, whereas the bis compounds 9aef were more effective with MICs between 0.2 and 12.5 μg/mL. Molecular modeling and 3DQSAR measurements using CoMFA and Topomer CoMFA further supported the observed results. The bis compound 9b showed excellent activity with MIC value as low as 0.2 μg/mL.
- Anand, Ashish,Naik, Reshma J.,Revankar, Hrishikesh M.,Kulkarni, Manohar V.,Dixit, Sheshagiri R.,Joshi, Shrinivas D.
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p. 194 - 207
(2015/11/03)
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- Practical and metal-free electrophilic aromatic halogenation by interhalogen compounds generated in situ from N-halosuccinimide and catalytic TMSCL
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Halomonochloride compounds (ClCl, BrCl, ICl) generated in situ from N-halosuccinimide and catalytic chlorotrimethylsilane (TMSCl, 0.1 equiv) can efficiently halogenate aromatic compounds to give halogenated products in good to excellent yields and selectivities. The reaction can be carried out at room temperature or at lower temperatures, requires only one hour, is practical to apply to a wide range of substrates, and provides a simple access to a variety of haloarene compounds. Georg Thieme Verlag Stuttgart New York.
- Maibunkaew, Tapanee,Thongsornkleeb, Charnsak,Tummatorn, Jumreang,Bunrit, Anon,Ruchirawat, Somsak
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supporting information
p. 1769 - 1775
(2014/08/05)
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- Indium-catalyzed intramolecular hydroarylation of aryl propargyl ethers
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Indium(iii) halides catalyze efficiently the intramolecular hydroarylation (IMHA) of aryl propargyl ethers. The reaction proceeds regioselectively with terminal and internal alkynes bearing electron-rich and electron-deficient substituents in the benzenes
- Alonso-Maran, Lorena,Martnez, M. Montserrat,Sarandeses, Luis A.,Sestelo, Jos Prez
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supporting information
p. 379 - 387
(2015/02/02)
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- Synthesis and biological evaluation of 4-(1,2,3-triazol-1-yl)coumarin derivatives as potential antitumor agents
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In this research, a series of 4-(1,2,3-triazol-1-yl)coumarin conjugates were synthesized and their anticancer activities were evaluated in vitro against three human cancer cell lines, including human breast carcinoma MCF-7 cell, colon carcinoma SW480 cell and lung carcinoma A549 cell. To increase the biological potency, structural optimization campaign was conducted focusing on the C-4 position of 1,2,3-triazole and the C-6, C-7 positions of coumarin. In addition, to further evaluate the role of 1,2,3-triazole and coumarin for antiproliferative activity, 9 compounds possessing 4-(piperazin-1-yl)coumarin framework and 3 derivatives baring quinoline core were also synthesized. By MTT assay in vitro, most of the compounds display attractive antitumor activities, especially 23. Further flow cytometry assays demonstrate that compound 23 exerts the antiproliferative role through arresting G2/M cell-cycle and inducing apoptosis.
- Zhang, Wenjuan,Li, Zhi,Zhou, Meng,Wu, Feng,Hou, Xueyan,Luo, Hao,Liu, Hao,Han, Xuan,Yan, Guoyi,Ding, Zhenyu,Li, Rui
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supporting information
p. 799 - 807
(2014/02/14)
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- Anticancer (hexacarbonyldicobalt)propargyl aryl ethers: Synthesis, antiproliferative activity, apoptosis induction, and effect on cellular oxidative stress
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While an increasing number of (hexacarbonyldicobalt)alkynes have been found to possess antiproliferative activity against a number of cancer cell lines, the role of the organometallic moiety in this bioactivity is not well understood. To gain a better und
- Schimler, Sydonie D.,Hall, David J.,Debbert, Stefan L.
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- Rapid access to chroman-3-ones through gold-catalyzed oxidation of propargyl aryl ethers
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The two-step: Chroman-3-ones are important intermediates for organic synthesis and medicinal chemistry. However, their syntheses require multiple steps and are not efficient. By using gold-catalyzed alkyne oxidation, this versatile heterocycle can be prepared in only two steps from readily available phenols and with mostly high efficiencies (see scheme).
- Wang, Yanzhao,Ji, Kegong,Lan, Sylvester,Zhang, Liming
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supporting information; experimental part
p. 1915 - 1918
(2012/03/26)
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- Gold nanoparticles supported on TiO2 catalyse the cycloisomerisation/oxidative dimerisation of aryl propargyl ethers
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Gold nanoparticles supported on TiO2 (~1%) catalyse in high yields the selective cycloisomerisation of aryl propargyl ethers into the corresponding 2H-chromenes, under heterogeneous conditions. 2H,2′H-3, 3′-Bichromenes resulting from a catalytic oxidative dimerization pathway are also formed as by-products. The Royal Society of Chemistry 2011.
- Efe, Christina,Lykakis, Ioannis N.,Stratakis, Manolis
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supporting information; experimental part
p. 803 - 805
(2011/04/12)
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- 4-Deoxy-4-fluoro-xyloside derivatives as inhibitors of glycosaminoglycan biosynthesis
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Various 4-deoxy-4-fluoro-xylosides were prepared using click chemistry for evaluating their potential utility as inhibitors of glycosaminoglycan biosynthesis. 2,3-Di-O-benzoyl-4-deoxy-4-fluoro-β-d-xylopyranosylazide, obtained from l-arabinopyranose by six
- Tsuzuki, Yasuhiro,Nguyen, Thao Kim Nu,Garud, Dinesh R.,Kuberan, Balagurunathan,Koketsu, Mamoru
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supporting information; experimental part
p. 7269 - 7273
(2011/01/12)
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- Intermolecular and intramolecular pauson-khand reactions of functionalized Allenes
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Pauson-Khand reactions of functionalized allenes with different alkynes give cyclopentenones with generally high regio-and stereoselectivities. The allenes react through their external double bonds, giving cyclopentenones with exocyclic double bond at their β positions and predominantly with E stereochemistry. Some intramolecular reactions with allenynes connected through aromatic rings are described. These give the corresponding heterocycles with moderate to good yields. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Gonzalez-Gomez, Alvaro,Anorbe, Loreto,Poblador, Amalia,Dominguez, Gema,Perez-Castells, Javier
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supporting information; experimental part
p. 1370 - 1377
(2009/04/11)
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- Natural products in parallel synthesis: Triazole libraries of nonactic acid
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The synthesis of a library of nonactic acid-derived triazoloamide derivatives and their evaluation as antimicrobial agents is described.
- Luesse, Sarah B.,Wells, Gregg,Nayek, Abhijit,Smith, Adrienne E.,Kusche, Brian R.,Bergmeier, Stephen C.,McMills, Mark C.,Priestley, Nigel D.,Wright, Dennis L.
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body text
p. 3946 - 3949
(2009/04/07)
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- Dioxane dibromide-mediated solvent-free synthesis of vicinal dibromides
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Structurally varied vicinal dibromides have been synthesized in high yield and good purity through highly stereoselective anti-addition of bromine across the olefinic linkages using dioxane dibromide (DD) under solvent-free conditions. Copyright Taylor & Francis Group, LLC.
- Chaudhuri, Subrata Kumar,Roy, Sanchita,Saha, Manabendra,Bhar, Sanjay
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p. 271 - 274
(2007/10/03)
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- Efficient synthesis of propargylic ethers under the DBU conditions and its application to natural products synthesis
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Conversion of dibromides carrying O-functional groups at adjacent positions to the corresponding propargylic ethers was successfully carried out under the DBU conditions through 2-bromo-1-alkenes as intermediates. The optically active γ-lactone-class natural products, such as (-)-muricatacin (4) and (R,R)-sapinofuranone B (5) were synthesized using the propargylic ether intermediate produced by the elimination reaction mentioned above.
- Yokoyama, Tadashi,Kutsumura, Noriki,Ohgiya, Tadaaki,Nishiyama, Shigeru
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p. 578 - 582
(2008/02/11)
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- 1,2-Dibromoalkanes into alkynes by elimination reaction under DBU conditions and their application to total synthesis of sapinofuranone B
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Treatment of 1,2-dibromoalkanes with DBU effected an elimination reaction, leading to the alkynes. Oxygen substitution at the C3 position plays a critical role to abstract protons by inductive effects. By the application of this protocol, a total synthesi
- Kutsumura, Noriki,Yokoyama, Tadashi,Ohgiya, Tadaaki,Nishiyama, Shigeru
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p. 4133 - 4136
(2007/10/03)
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- A hierarchy of aryloxide deprotection by boron tribromide
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Aryl propargyl ethers and esters are cleaved selectively in the presence of aryl methyl ethers and esters by boron tribromide in dichloromethane. Under the same conditions, allyl ethers undergo very rapid Claisen rearrangement, and benzyl ethers are also cleaved more rapidly than propargyl. A mechanism involving intramolecular delivery of bromide to the propargyl terminus is proposed.
- Punna, Sreenivas,Meunier, Stephane,Finn
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p. 2777 - 2779
(2007/10/03)
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- Cardioselective Antiischemic ATP-Sensitive Potassium Channel Openers. 2. Structure-Activity Studies on Benzopyranylcyanoguanidines: Modification of the Benzopyran Ring
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The ATP-sensitive potassium channel (KATP) openers are of considerable interest as myocardial protecting agents.However, there exists a narrow window of safety for the use of first-generation compounds as antiischemic agents due to their powerf
- Atwal, Karnail S.,Grover, Gary J.,Ferrara, Francis N.,Ahmed, Syed Z.,Sleph, Paul G.,et al.
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p. 1966 - 1973
(2007/10/02)
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