- The polymorphism of porphyrin 2D assemblies at the liquid-graphite interface: The effect of a polar solvent additive and a flexible spacer on the face-on and edge-on type molecular arrangements
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Self-assembly structures of 5,10,15,20-tetrakis(4-substituted phenyl)porphyrins at the liquid-graphite interface were investigated by scanning tunneling microscopy. We found that the presence of a small amount of a polar solvent, i.e., only 0.5 vol% of octanoic acid in phenyloctane, significantly affected the selective formation of the face-on polymorph over the edge-on one likely due to the solvent-molecule interactions at the 2D interface.
- Adachi, Kenya,Hirose, Takashi,Matsuda, Kenji
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- SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
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- Selective oxoammonium salt oxidations of alcohols to aldehydes and aldehydes to carboxylic acids
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The oxidation of alcohols to aldehydes using stoichiometric 4-acetamido-2,2,6,6-tetramethylpiperidine-1-oxoammonium tetrafluoroborate (1) in CH2Cl2 at room temperature is a highly selective process favoring reaction at the carbinol center best able to accommodate a positive charge. The oxidation of aldehydes to carboxylic acids by 1 in wet acetonitrile is also selective; the rate of the process correlates with the concentration of aldehyde hydrate. A convenient and high yield method for oxidation of alcohols directly to carboxylic acids has been developed.
- Qiu, Joseph C.,Pradhan, Priya P.,Blanck, Nyle B.,Bobbitt, James M.,Bailey, William F.
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supporting information; experimental part
p. 350 - 353
(2012/03/09)
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- Chemoselective conversion of α-unbranched aldehydes to amides, esters, and carboxylic acids by NHC-catalysis
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Depending on the N-heterocyclic carbene catalyst utilized, α-unbranched aldehydes selectively provided amides, esters, or carboxylic acids through oxidation by NCS. The α-unbranched aldehyde underwent these reactions chemoselectively in the presence of an aromatic or α-branched aldehyde.
- Kuwano, Satoru,Harada, Shingo,Oriez, Raphael,Yamada, Ken-Ichi
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supporting information; experimental part
p. 145 - 147
(2012/01/12)
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- NOVEL THIOPHENE DERIVATIVES AS SPHINGOSINE-1-PHOSPHATE-1 RECEPTOR AGONISTS
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The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
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- Rhodium(I)-catalyzed 1,4-addition of arylboronic acids to acrylic acid in water: One-step preparation of 3-arylpropionic acids
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A practical method for the one-step preparation of 3-arylpropionic acids through rhodium-catalyzed 1,4-addition of arylboronic acids to acrylic acid is reported. The method is applicable to a broad scope of aryl boronic acids and displays a wide functional group tolerance operating in water as the optimal reaction medium. Georg Thieme Verlag Stuttgart · New York.
- Vautravers, Nicolas R.,Breit, Bernhard
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supporting information; experimental part
p. 2517 - 2520
(2011/11/12)
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- N-Hydroxy-(4-oxime)-cinnamide: A versatile scaffold for the synthesis of novel histone deacetilase (HDAC) inhibitors
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With the aim to discover novel HDAC inhibitors with high potency and good safety profiles, we have designed a small library based on a N-hydroxy-(4-oxime)-cinnamide scaffold. We describe the synthesis of these novel compounds and some preliminary in vitro
- Giannini, Giuseppe,Marzi, Mauro,Pezzi, Riccardo,Brunetti, Tiziana,Battistuzzi, Gianfranco,Marzo, Maria Di,Cabri, Walter,Vesci, Loredana,Pisano, Claudio
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scheme or table
p. 2346 - 2349
(2009/12/07)
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- HDAC INHIBITORS
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Compounds of formula (I) inhibit HDAC activity, wherein A, B and D independently represent =C- or =N-; W is a divalent radical -CH=CH- or CH2CH2-; R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.
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- Cinnamic, Phenylpropiolic and Phenylpropanoic Acid Derivatives Useful as Anti-Tumor Agents
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Cinnamic and phenylpropiolic acid derivatives of formula (I) having antitumour and chemo sensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.
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Page/Page column 10
(2008/12/07)
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- Novel Thiophene Derivatives as Spingosine-1-Phosphate-1 Receptor Agonists
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The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
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Page/Page column 22
(2008/12/07)
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- CINNAMIC, PHENYLPROPIOLIC AND PHENYLPROPANOIC ACID DERIVATIVES USEFUL AS ANTI-TUMOUR AGENTS
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Cinnamic and phenylpropiolic acid derivatives of Formula (I) having antitumour and chemosensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.
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- CBI analogues of the duocarmycins and CC-1065
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An extensive series of CBI analogues of the duocarmycins and CC-1065 exploring substituent effects within the first indole DNA binding subunit is detailed. In general, substitution at the indole C5 position led to cytotoxic potency enhancements that can be ≧1000-fold providing simplified analogues containing a single DNA binding subunit that are more potent (IC50=2-3 pM) than CBI-TMI, duocarmycin SA, or CC-1065. The increases in cytotoxicity correlate well with accompanying increases in the rate and efficiency of DNA alkylation. This effect is more pronounced with the CBI versus DSA or CPI based analogues. Moreover, this effect is largely insensitive to the electronic character of the C5 substituent but is sensitive to the size, rigid length, and shape (sp, sp2, sp3 hybridization) of this substituent consistent with expectation that the impact is due simply to its presence.
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- Direct synthesis of 3-arylpropionic acids by tetraphosphine/palladium catalysed Heck reactions of aryl halides with acrolein ethylene acetal
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Through the use of [PdCl(C3H5)]2/Cis,cis, cis-1,2,3,4-tetrakis(diphenylphosphinomethyl)cyclopentane as a catalyst, a range of aryl bromides undergoes Heck reaction with acrolein ethylene acetal. With this acetal, the selective formation of 3-arylpropionic acids/esters was observed. The functional group tolerance on the aryl halide is remarkable; substituents such as fluoro, methyl, methoxy, acetyl, formyl, benzoyl, nitro or nitrile are tolerated. Furthermore, this catalyst can be used at low loading, even for reactions of sterically hindered aryl bromides. Graphical Abstract.
- Lemhadri, Mhamed,Doucet, Henri,Santelli, Maurice
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p. 11533 - 11540
(2007/10/03)
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- Enediyne derivatives useful for the synthesis of conjugates of methyltrithio antitumor agents
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This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.
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- A combinatorial protecting group strategy for oligonucleotide synthesis
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A novel 5'-3' directed DNA synthesis will be described. Together with additional investigations on model compounds a synthetic strategy is established which allows multiselective deprotections. This offers the potential to either generate oligonucleotides in different sequence specific protection/functionalization states or to create a combinatorial set of molecules available for specific molecular interaction of recognition experiments.
- Leikauf, Eckart,Barnekow, Frank,Koester, Hubert
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p. 6913 - 6930
(2007/10/03)
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- Fluorogenic 2-oxy-3(2H)-furanone materials
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Compounds of the formula SPC1 Wherein R1 is lower alkyl or phenyl lower alkyl; R2 is phenyl or substituted phenyl; and R3 is substituted or unsubstituted phenyl, naphthyl or indolyl; Are fluorogenic reagents which react wi
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