- Synthesis of chiral helical poly(hydroxyl-containing phenylacetylene) membranes by in-situ depinanylsilylation and their enantioselective permeabilities
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Two new chiral helical poly(hydroxyl-containing phenylacetylene) membranes without the coexistence of any other chiral moieties were prepared in the following manner: (1) synthesis and homo-or copolymerization of two new chiral pinanylsiloxy-containing ph
- Teraguchi, Masahiro,Mottate, Kazuomi,Kim, Sun-Young,Aoki, Toshiki,Kaneko, Takashi,Hadano, Shingo,Masuda, Toshio
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Read Online
- A Helical Polyphenylacetylene Having Amino Alcohol Moieties Without Chiral Side Groups as a Chiral Ligand for the Asymmetric Addition of Diethylzinc to Benzaldehyde
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One-handed helical polyphenylacetylenes having achiral amino alcohol moieties, but no chiral side groups, were synthesized by the helix-sense-selective copolymerization of an achiral phenylacetylene having an amino alcohol side group with a phenylacetylene having two hydroxyl groups. Since the resulting helical copolymers were successfully utilized as chiral ligands for the enantioselective alkylation of benzaldehyde with diethylzinc, we can conclude that the main-chain chirality based on the one-handed helical conformation is useful for the chiral catalysis of an asymmetric reaction for the first time. The enantioselectivities of the reaction were controlled by the optical purities of the helical polymer ligands. In addition, the polymer ligands could be easily recovered by precipitation after the reaction. Chirality 27:454-458, 2015.
- Liu, Lijia,Long, Qing,Aoki, Toshiki,Zhang, Geng,Kaneko, Takashi,Teraguchi, Masahiro,Zhang, Chunhong,Wang, Yudan
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Read Online
- Synthesis of siRNAs incorporated with cationic peptides R8G7 and R8A7 and the effect of the modifications on siRNA properties
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Small interfering RNA (siRNA) can be used as an innovative next-generation drug. However, there are several challenges in the therapeutic application of siRNAs, including their low cell membrane permeability. In this study, we designed and synthesized siR
- Honda, Kenji,Kajino, Ryohei,Kakisawa, Yuri,Maeda, Yusuke,Matsubara, Miho,Ozaki, Koki,Ueno, Yoshihito
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Read Online
- Synthesis of a fluorescent BODIPY-tagged ROMP catalyst and initial polymerization-propelled diffusion studies
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Abstract The synthesis of a Ru-based olefin metathesis catalyst dye-tagged at the N-heterocyclic carbene ligand is reported. Its catalytic activity toward ring-opening metathesis polymerization (ROMP) of 1,5-cyclooctadiene was found to be similar to that
- Godoy, Jazmin,García-López, Víctor,Wang, Lin-Yung,Rondeau-Gagné, Simon,Link, Stephan,Martí, Angel A.,Tour, James M.
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Read Online
- Visible light-induced heterogeneous Meerwein-Ponndorf-Verley-type reduction of an aldehyde group over an organically modified titanium dioxide photocatalyst
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An organically modified titanium dioxide photocatalyst prepared by a simple impregnation method chemoselectively and almost quantitatively converted benzaldehydes having other reducible functional groups to the corresponding benzyl alcohols under visible
- Fukui, Makoto,Tanaka, Atsuhiro,Hashimoto, Keiji,Kominami, Hiroshi
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Read Online
- Design, synthesis and antitumor evaluations of nucleoside base hydroxamic acid derivatives as DNMT and HDAC dual inhibitors
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DNA methyltransferase (DNMT) and histone deacetylase (HDAC) are well recognized epigenetic targets for discovery of antitumor agents. In this study, we designed and synthesized a series of nucleoside base hydroxamic acid derivatives as DNMT and HDAC dual inhibitors. MTT assays and enzymatic inhibitory activity tests indicated that compound 204 exhibited potent DNMT1 and HDAC1/6 inhibitory potency simultaneously in enzymatic levels and at cellular levels, inducing hypomethylation of p16 and hyperacetylation of histones H3K9 and H4K8. Besides, 204 remarkably inhibited proliferation against cancer cells U937 by prompting G0/G1 cell cycle arrest. Molecular docking models explained the functional mechanism of 204 inhibiting DNMT1 and HDAC. Preliminary studies on metabolic profiles revealed that 204 showed desirable stability in liver microsomes. Our study suggested that 204 inhibiting DNMT and HDAC concurrently can be a potential lead compound for epigenetic cancer therapy.
- Sun, Qinsheng,Dai, Qiuzi,Zhang, Cunlong,Chen, Yan,Zhao, Lei,Yuan, Zigao,Jiang, Yuyang
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Read Online
- Creating Dynamic Nanospaces in Solution by Cationic Cages as Multirole Catalytic Platform for Unconventional C(sp)?H Activation Beyond Enzyme Mimics
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Herein we demonstrate that, based on the creation of dynamic nanospaces in solution by highly charged positive coordination cage of [Pd6(RuL3)8]28+, multirole and multi-way cage-confined catalysis is accomplisha
- Li, Kang,Wu, Kai,Lu, Yu-Lin,Guo, Jing,Hu, Peng,Su, Cheng-Yong
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supporting information
(2021/12/14)
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- Electrochemical Difunctionalization of Terminal Alkynes: Access to 1,4-Dicarbonyl Compounds
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1,4-Dicarbonyl compounds are versatile scaffolds for the heterocycle synthesis, including the Paal-Knorr reaction. Herein, a feasible electrosynthesis method to access 1,4-dicarbonyl compounds has been developed from simple alkynes and 1,3-dicarbonyl compounds. When the undivided cell is combined with the constant current mode, aryl alkynes containing numerous medicinal motifs with 1,3-dicarbonyl esters or ketones react smoothly. External oxidant and catalyst-free conditions conform to the requirements of green synthesis.
- Hu, Jingcheng,Zeng, Li,Hu, Jiayu,Ma, Rui,Liu, Xue,Jiao, Ying,He, Haoyu,Chen, Siyu,Xu, Zhexi,Wang, Hongfei,Lei, Aiwen
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supporting information
p. 289 - 292
(2022/01/04)
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- ANTIBACTERIAL AND ANTIFUNGAL PLEUROMUTILIN CONJUGATES
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Compounds of formula (1) comprising a pleuromutilin backbone with a triazole based side-group at C22 are provided. The compounds can be used for treatment of bacterial infections and fungal infections. Importantly, infections caused by multidrug-resistant
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Page/Page column 26; 29
(2021/11/06)
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- Iron-Catalyzed Tertiary Alkylation of Terminal Alkynes with 1,3-Diesters via a Functionalized Alkyl Radical
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Direct oxidative C(sp)?H/C(sp3)?H cross-coupling offers an ideal and environmentally benign protocol for C(sp)?C(sp3) bond formations. As such, reactivity and site-selectivity with respect to C(sp3)?H bond cleavage have remained a persistent challenge. Herein is reported a simple method for iron-catalyzed/silver-mediated tertiary alkylation of terminal alkynes with readily available and versatile 1,3-dicarbonyl compounds. The reaction is suitable for an array of substrates and proceeds in a highly selective manner even employing alkanes containing other tertiary, benzylic, and C(sp3)?H bonds alpha to heteroatoms. Elaboration of the products enables the synthesis of a series of versatile building blocks. Control experiments implicate the in situ generation of a tertiary carbon-centered radical species.
- Tian, Ming-Qing,Shen, Zhen-Yao,Zhao, Xuefei,Walsh, Patrick J.,Hu, Xu-Hong
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supporting information
p. 9706 - 9711
(2021/03/19)
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- Copper-catalyzed formal transfer hydrogenation/deuteration of aryl alkynes
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A copper-catalyzed reduction of alkynes to alkanes and deuterated alkanes is described under transfer hydrogenation and transfer deuteration conditions. Commercially available alcohols and silanes are used interchangeably with their deuterated analogues as the hydrogen or deuterium sources. Transfer deuteration of terminal and internal aryl alkynes occurs with high levels of deuterium incorporation. Alkyne-containing complex natural product analogues undergo transfer hydrogenation and transfer deuteration selectively, in high yield. Mechanistic experiments support the reaction occurring through a cis-alkene intermediate and demonstrate the possibility for a regioselective alkyne transfer hydrodeuteration reaction.
- Sloane, Samantha E.,Reyes, Albert,Vang, Zoua Pa,Li, Lingzi,Behlow, Kiera T.,Clark, Joseph R.
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supporting information
p. 9139 - 9144
(2020/11/30)
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- Synthesis and biological evaluation of PF-543 derivative
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PF-543 has been known as a substance that strongly inhibits SK1. However, it also exhibits antineoplastic activity that is lower than other inhibitors of SK1. In this study, we compared PF-543 and synthesized a newly designed derivative of PF-543 (compoun
- Kim, Seon Woong,Lee, Taeho,Lee, Joo-Youn,Kim, Sanghee,Jun, Hee-Sook,Park, Eun-Young,Baek, Dong Jae
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supporting information
p. 2 - 5
(2019/05/04)
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- Visible-Light-Induced [4+2] Annulation of Thiophenes and Alkynes to Construct Benzene Rings
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The [4+2] annulation represents an elegant and versatile synthetic protocol for the construction of benzene rings. Herein, a strategy for visible-light induced [4+2] annulation of thiophenes and alkynes, to afford benzene rings, is presented. Under simple and mild reaction conditions, the ready availability and structural diversity of thiophenes and alkynes permit the facile synthesis of several substituted aromatic rings. Valuable drugs and amino acids are also well tolerated. Moreover, DFT calculations explain the high regioselectivity of the reaction.
- Song, Chunlan,Dong, Xin,Wang, Zhongjie,Liu, Kun,Chiang, Chien-Wei,Lei, Aiwen
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supporting information
p. 12206 - 12210
(2019/07/31)
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- APOPTOSIS INHIBITORS
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The invention provides compounds that are inhibitors or covalent modifiers of succinate dehydrogenase subunit B (SDHB) and/or inhibitors of apoptosis, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition.
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Paragraph 0364
(2018/02/27)
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- INDOLINONE DERIVATIVES AS INHIBITORS OF MATERNAL EMBRYONIC LEUCINE ZIPPER KINASE
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The present disclosure relates to indolinone compounds, compositions, and methods for the inhibition of maternal embryonic leucine zipper kinase (MELK). The present disclosure further relates to indolinone compounds, compositions, and methods for the treatment or prevention of a cancer (for example, triple negative breast cancer).
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Page/Page column 87-88
(2018/09/20)
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- Design and Synthesis of Quenched Activity-based Probes for Diacylglycerol Lipase and α,β-Hydrolase Domain Containing Protein 6
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Diacylglycerol lipases (DAGL) are responsible for the biosynthesis of the endocannabinoid 2-arachidonoylglycerol. The fluorescent activity-based probes DH379 and HT-01 have been previously shown to label DAGLs and to cross-react with the serine hydrolase ABHD6. Here, we report the synthesis and characterization of two new quenched activity-based probes 1 and 2, the design of which was based on the structures of DH379 and HT-01, respectively. Probe 1 contains a BODIPY-FL and a 2,4-dinitroaniline moiety as a fluorophore–quencher pair, whereas probe 2 employs a Cy5-fluorophore and a cAB40-quencher. The fluorescence of both probes was quenched with relative quantum yields of 0.34 and 0.0081, respectively. The probes showed target inhibition as characterized in activity-based protein profiling assays using human cell- and mouse brain lysates, but were unfortunately not active in living cells, presumably due to limited cell permeability.
- van Rooden,Kohsiek,Kreekel,van Esbroeck,van den Nieuwendijk,Janssen,van den Berg,Overkleeft,van der Stelt
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p. 3491 - 3500
(2018/11/25)
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- Sensor with a scaffold having changeable conformations
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The present invention relates to a scaffolded sensor with a container comprising a drug for triggering drug release, wherein the scaffold is intrinsically conformationally metastable and a method to its manufacture.
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Page/Page column 19; 20; 26; 27
(2017/09/26)
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- SILICON BASED DRUG CONJUGATES AND METHODS OF USING SAME
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Described herein are silicon based conjugates capable of delivering one or more payload moieties to a target cell or tissue. Contemplated conjugates may include a silicon-heteroatom core, one or more optional catalytic moieties, a targeting moiety that permits accumulation of the conjugate within a target cell or tissue, one or more payload moieties (e.g., a therapeutic agent or imaging agent), and two or more non-interfering moieties covalently bound to the silicon-heteroatom core.
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Paragraph 0728; 0733; 0734
(2017/08/07)
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- Application of polymer microspheres to Raman detection
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The invention discloses application of polymer microspheres to Raman detection. Methacrylate/amide polymer monomers or styrene polymer monomers containing alkynyl, cyano, azido or a carbon-deuterium bond group are prepared into the polymer microspheres with the particle diameter from a nanometer grade to a micron grade through an emulsion polymerization or dispersion polymerization method; the polymer microspheres have a remarkable Raman signal under the condition of no metal sensitization structure; and a Raman characteristic peak signal is located in a Raman quiet zone (1800cm to 2800cm) in a living organism and can be used as a marker for biological imaging.
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Paragraph 0115; 0126-0128
(2018/03/13)
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- Nucleoside and base hydroxamic acid derived compound and preparation method and applications thereof
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The invention discloses a nucleoside and base hydroxamic acid compound with DNA transmethylase and/or histone deacetylase inhibition activity, and a preparation method and applications thereof. The structural formula of the nucleoside and base hydroxamic acid compound is shown as the formula I, wherein R is nucleoside and base, nucleoside and base with substituent group or nucleoside and base analogue in DNA and/or RNA; Linker is a connecting chain connecting R with hydroxamic acid function group, the connecting chain comprises but is not limited within alkyl chain, alkyl chain with heteroatom, alkyl chain with aromatic ring, and alkyl chain with heterocycle. In-vitro cell proliferation assay show that the compound shown in the formula I can well inhibit the proliferation of leukemia cell K562 and histocyte lymphoma cell U937. Transmethylase and histone deacetylase inhibition assay shows that the compound shown in the formula I is a compound having inhibition activity on the DNA transmethylase and/or histone deacetylase. The formula I is as shown in the specification.
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Paragraph 0186
(2017/08/29)
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- Pyrimidine or pyridine pyridine ketone compound and its preparation method and application (by machine translation)
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The invention discloses a kind of type I of the pyrimidine or pyridine pyridine ketone compound and its preparation and application, which belongs to the technical field of pharmaceutical preparation. The compounds have high-efficient and selectively inhibit the cell cycle dependent kinases (Cdks) CDK4 and CDK6 active, and then by inhibiting CDK4/CDK6 prevent tumor cell division. Therefore, the compounds of this invention can be used for CDK4 and CDK6 the involved in cell cycle control disorders result in various diseases, especially suitable for the treatment of malignant tumors. (by machine translation)
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Paragraph 0328
(2016/10/09)
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- A copper (II) (II) composite chlorinating agent and copper-based composite chlorinating agent synthesis of 1-chloro-2-aryl acetylene method
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The invention discloses a copper (II) composite chlorinating agent and a method for synthesizing 1-chlorine-2-aryl acetylene based on the copper (II) composite chlorinating agent. The structural formula of the copper (II) composite chlorinating agent is CuCl2.xNaCl.yAl2O3. The chlorinating agent is applicable to chlorination of various substituted aryl acetylene substrates, and is high in universality; the chlorinating agent can directly carry out chlorination reaction on aryl acetylene so as to obtain a 1-chlorine-2-aryl acetylene product; the method is mild in reaction condition, 1-chlorine-2-aryl acetylene can be synthesized with high yield and high selectivity, and the production cost of the 1-chlorine-2-aryl acetylene derivative is greatly lowered.
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Paragraph 0092; 0153; 0154
(2016/11/24)
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- Exploring the synthesis and the reactivity of 4-[4-(chloromethyl)styryl]-1, 2-dimethyl-5-nitro-1H-imidazole in TDAE strategy
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We describe herein the preparation of 4-[4-(chloromethyl)styryl]-1,2- dimethyl-5-nitro-1H-imidazole via a Stille cross-coupling reaction. After determining the best reaction conditions, we investigated the reactivity of this activated chloromethyl compoun
- Primas, Nicolas,Neildé, Kévin,Kabri, Youssef,Crozet, Maxime D.,Terme, Thierry,Vanelle, Patrice
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p. 348 - 356
(2014/02/14)
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- Air-stable gold nanoparticles ligated by secondary phosphine oxides for the chemoselective hydrogenation of aldehydes: Crucial role of the ligand
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The synthesis of air-stable and homogeneous gold nanoparticles (AuNPs) employing tert-butyl(naphthalen-1-yl)phosphine oxide as supporting ligand is described via NaBH4 reduction of a Au(I) precursor, [(tert-butyl(naphthalen-1-yl)phosphine oxide)AuCl]2. This highly reproducible and simple procedure furnishes small (1.24 ± 0.16 nm), highly soluble nanoparticles that are found to be highly active catalysts for the hydrogenation of substituted aldehydes, giving high conversions and chemoselectivities for a wide variety of substrates. In addition to catalytic studies the role of the novel stabilizer in the remarkable activity and selectivity exhibited by this system was interrogated thoroughly using a wide range of techniques, including ATR FT-IR, HRMAS NMR, XPS, and EDX spectroscopy. In particular, isotopic labeling experiments enabled us to probe the coordination mode adopted by the SPO ligand bound to the nanoparticle surface by ATR FT-IR spectroscopy. In combination with a series of control experiments we speculate that the SPO ligand demonstrates ligand-metal cooperative effects and plays a seminal role in the heterolytic hydrogenation mechanism.
- Cano, Israel,Chapman, Andrew M.,Urakawa, Atsushi,Van Leeuwen, Piet W. N. M.
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supporting information
p. 2520 - 2528
(2014/03/21)
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- Redox-selective generation of aldehydes and H2 from alcohols under visible light
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Photosynthetic dehydrogenation: Potential usefulness of visible-light-induced dehydrogenation of alcohols in organic synthesis was demonstrated, in which aldehydes and H2 were afforded by using Ru/SrTiO3:Rh and water (see scheme). Water was essential for the reaction. High efficiency (TON: up to 15 400 based on Rh; H2 and aldehyde evenly generated) and high selectivity were achieved. Copyright
- Liu, Zijun,Caner, Joaquim,Kudo, Akihiko,Naka, Hiroshi,Saito, Susumu
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supporting information
p. 9452 - 9456
(2013/07/26)
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- SENSOR
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The present invention relates to a scaffolded sensor with a container comprising a drug for triggering drug release, wherein the scaffold is intrinsically conformationally metastable and a method to its manufacture.
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Page/Page column
(2013/10/22)
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- HISTONE DEACETYLASE INHIBITORS
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The disclosure provides compounds of formula I and methods for preparation thereof. The compounds act as inhibitor of histone deacetylase.
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Page/Page column 12
(2012/05/04)
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- HISTONE DEACETYLASE INHIBITORS
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The disclosure provides compounds of formula I and methods for preparation thereof. The compounds act as inhibitor of histone deacetylase.
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Page/Page column 35; 36
(2011/04/13)
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- N-[2-methyl-5-(triazol-1-yl)phenyl]pyrimidin-2-amine as a Scaffold for the synthesis of inhibitors of Bcr-Abl
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N-[2-Methyl-5-(triazol-1-yl)phenyl]pyrimidin-2-amine derivatives were synthesized and evaluated invitro for their potential use as inhibitors of Bcr-Abl. The design is based on the bioisosterism between the 1,2,3-triazole ring and the amide group. The synthesis involves a copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) as the key step, with the exclusive production of anti-(1,4)-triazole derivatives. One of the compounds obtained shows general activity similar to that of imatinib; in particular, it was observed to be more effective in decreasing the fundamental function of cdc25A phosphatases in the K-562 cell line. Willing and Abl inhibitors! N-[2-Methyl-5-(triazol-1-yl)phenyl]pyrimidin-2-amine derivatives were synthesized by a copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) as a key step, with anti-(1,4)-triazole derivatives as the exclusive products. One of these compounds shows general activity similar to that of imatinib, and in particular, it is more effective in decreasing the fundamental function of cdc25A phosphatases in the K-562 cell line.
- Arioli, Federica,Borrelli, Stella,Colombo, Francesco,Falchi, Federico,Filippi, Irene,Crespan, Emmanuele,Naldini, Antonella,Scalia, Giusy,Silvani, Alessandra,Maga, Giovanni,Carraro, Fabio,Botta, Maurizio,Passarella, Daniele
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experimental part
p. 2009 - 2018
(2012/06/30)
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- Synthesis and antiplasmodial activity of new indolone N-Oxide derivatives
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A series of 66 new indolone-N-oxide derivatives was synthesized with three different methods. Compounds were evaluated for in vitro activity against CQ-sensitive (3D7), CQ-resistant (FcB1), and CQ and pyrimethamine cross-resistant (K1) strains of Plasmodium falciparum (P.f.), aswell as for cytotoxic concentration (CC50) on MCF7 and KB human tumor cell lines. Compound 26 (5-methoxy-indolone-N-oxide analogue) had the most potent antiplasmodial activity in vitro (50 MCF7/IC50 FcB1: 14623; CC50 KB/IC50 3D7: 198823). In in vivo experiments, compound 1 (dioxymethylene derivatives of the indolone-N-oxide) showed the best antiplasmodial activity against Plasmodium berghei, 62% inhibition of the parasitaemia at 30 mg/kg/day. 2009 American Chemical Society.
- Nepveu, Fran?oise,Kim, Sothea,Boyer, Jeremie,Chatriant, Olivier,Ibrahim, Hany,Reybier, Karine,Monje, Marie-Carmen,Chevalley, Severine,Perio, Pierre,Lajoie, Barbora H.,Bouajila, Jalloul,Deharo, Eric,Sauvain, Michel,Tahar, Rachida,Basco, Leonardo,Pantaleo, Antonella,Turini, Francesco,Arese, Paolo,Valentin, Alexis,Thompson, Eloise,Vivas, Livia,Petit, Serge,Nallet, Jean-Pierre
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scheme or table
p. 699 - 714
(2010/07/09)
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- Weak interactions dominating the supramolecular self-assembly in a salt: A designed single-crystal-to-single-crystal topochemical polymerization of a terminal aryldiacetylene
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Single-crystal-to-single-crystal (SCSC) topochemical polymerizations of diacetylenes can yield nearly defect-free conjugated polymer crystals unattainable by other methods. Aryl-substituted diacetylenes with their potentially greater conjugation have been targeted for years, but until now no one has reported a SCSC polymerization of any aryl-substituted diacetylene. This is presumably due to the rigidity of such diaryl-substituted monomers as well as the lack of control over the supramolecular structure. To address this problem, the polymerization of a terminal phenyldiacetylene was targeted. It was assumed that a terminal diacetylene should demonstrate greater flexibility in the solid state. To establish the necessary (~4.9 A) repeat distance, commensurate with the repeat distance in the polymer, a host-guest system was designed. The chosen diacetylene guest, the amine DABzNH2, was to be crystallized with the oxalamide dicarboxylic acid host, H2og. The plan required a segregation of the hydrogen bonds, amide-amide hydrogen bonds to establish the 4.9 A spacing, and the carboxylate to ammonium ion hydrogen bonds to organize the guest. Prior to carrying out the diacetylene synthesis a series of model salts were studied. Consistent with the hydrophobic effect it was found that amines with large "greasy" substituents assembled according to the design. Once the model studies established that weak interactions could dominate the supramolecular structure of a salt, the actual design was put to the test. The targeted guest, DABzNH2, was synthesized and crystals of the host-guest salt (DABzNH3) 2og were prepared. The resulting crystal structure was in complete accordance with the design. A SCSC polymerization was achieved by a slow annealing treatment lasting about three months. The crystal structure of the resulting polymer not only confirmed the first example of a poly(aryldiacetylene) single crystal, it also revealed an unexpected reaction pathway that shows a major movement involving the rigid aromatic substituent.
- Li, Zhong,Fowler, Frank W.,Lauher, Joseph W.
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supporting information; experimental part
p. 634 - 643
(2009/06/18)
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- Revisiting the Meerwein-Ponndorf-Verley reduction: A sustainable protocol for transfer hydrogenation of aldehydes and ketones
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An economical and sustainable transfer hydrogenation for aldehydes and ketones is described. The general protocol is mild, chemo-selective and, importantly, uses neither precious nor non-precious metals and even no ligands. The Royal Society of Chemistry 2009.
- Polshettiwar, Vivek,Varma, Rajender S.
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experimental part
p. 1313 - 1316
(2010/05/02)
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- Facile deprotection of bulky (trialkylsilyl)acetylenes with silver fluoride
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An efficient and mild method is developed for the deprotection of bulky (trialkylsilyl)acetylenes. Treatment of 1-(triisopropylsilyl) acetylenes with silver fluoride, followed by hydrolysis of the intermediate silver acetylide with organic or inorganic ac
- Kim, Sanghee,Kim, Bogyeong,In, Jinkyung
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experimental part
p. 1963 - 1968
(2009/12/27)
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- ACETYLENIC COMPOUNDS
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The present invention relates to a class of acetylenic compounds, to a method of preparing the acetylenic compounds, and to the polymerisation and therapeutic uses of the acetylenic compounds. The invention particularly relates to compounds containing two acetylenic moieties.
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Page/Page column 65
(2008/06/13)
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- Novel synthetic luteolin analogue-caused sensitization of tumor necrosis factor-α-induced apoptosis in human tumor cells
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Studies on the sensitization, by novel alkynyl luteolin analogues, of TNF-α-induced apoptosis in HeLa and HepG2 cells revealed that LA-12 showed better sensitizing effects on TNF-α-induced cell death than luteolin, suggesting great potential for alkynyl luteolin analogues in cancer therapy.
- Cheng, Lili,Tan, Huiling,Wu, Xiaoyu,Hu, Ruijun,Aw, Carlin,Zhao, Min,Shen, Han-Ming,Lu, Yixin
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supporting information; experimental part
p. 4102 - 4104
(2009/02/07)
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- Thermoreversible cis-cisoidal to cis-transoidal isomerization of helical dendronized polyphenylacetylenes
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High cis content (81-99%) cis-transoidal polyphenylacetylene (PPA) jacketed with amphiphilic self-assembling dendrons, poly[(3,4-3,5)mG2-4EBn] with m = 8, 10, 12, 14, 16, and (S)-3,7-dimethyloctyl, were synthesized by Rh(C≡CPh)(nbd)(PPh3)2
- Percec, Virgil,Rudick, Jonathan G.,Peterca, Mihai,Wagner, Martin,Obata, Makoto,Mitchell, Catherine M.,Cho, Wook-Dong,Balagurusamy, Venkatachalapathy S. K.,Heiney, Paul A.
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p. 15257 - 15264
(2007/10/03)
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- A molecular ball bearing mediated by multiligand exchange in concert
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A thrust in the right direction: Two different disk-shaped ligands (a tris-monodentate and a hexa-monodentate ligand) and three Ag+ ions have been used as bearings and balls, respectively, in the construction of a molecular thrust ball bearing
- Hiraoka, Shuichi,Hirata, Kaori,Shionoya, Mitsuhiko
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p. 3814 - 3818
(2007/10/03)
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- Cross-coupling of aryl iodides with paramagnetic terminal acetylenes derived from 4,4,5,5-tetramethyl-2-imidazoline-2-oxyl 3-oxide
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2-(Arylylethynylphenyl)-4,4,5,5-tetramethyl-2-imidazoline-1-oxyl 3-oxides 12 and 13 were synthesized by cross-coupling of aryl iodides with 1-alkynes containing the 4,4,5,5-tetramethyl-2-imidazoline-1-oxyl 3-oxide fragment. A procedure was developed for the preparation of 3-and 4-ethynyibenzaldehydes with the use of 2-methylbut-3-yn-2-ol.
- Klyatskaya, S. V.,Tretyakov, E. V.,Vasilevsky, S. F.
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p. 128 - 134
(2007/10/03)
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- Synthesis of chiral dendrimers with a hydrocarbon backbone and application to the catalytic enantioselective addition of dialkylzincs to aldehydes
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Chiral dendrimers with three or six β-amino alcohols on hyperbranched hydrocarbon chain-ends were synthesized. These macromolecules can act as chiral catalysts for the enantioselective addition of dialkylzincs to aldehydes. The corresponding secondary alc
- Sato, Itaru,Shibata, Takanori,Ohtake, Koji,Kodaka, Ryo,Hirokawa, Yutaka,Shirai, Nobuaki,Soai, Kenso
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p. 3123 - 3126
(2007/10/03)
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- The Synthesis of Aromatic Leukotriene Analogues; Regioselective Trapping of 2,4'-Dilithiophenylethyne
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The 8,11-bridged aromatic leukotriene B4 analogues (3), (4), and (5), in which conformational freedom is restricted, have been prepared by extremely short synthetic routes.Conditions are described which allow the regioselective electrophillic t
- Furber, Mark,Taylor, Richard J. K.,Burford, S. Cliff
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p. 1573 - 1578
(2007/10/02)
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