- Innovative Multipodal Ligands Derived from Tr?ger's Bases for the Sensitization of Lanthanide(III) Luminescence
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Herein, the synthesis and characterization of the first family of multipodal ligands with a Tr?ger's base framework designed for the preparation of luminescent lanthanide(III) complexes are reported. Eight ligands were designed and synthesized using diffe
- Barja, Beatriz C.,Bruttomesso, Andrea C.,Eliseeva, Svetlana V.,Petoud, Stéphane,Ramírez, Javier A.,Trupp, Leandro,Vardé, Mariana
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supporting information
p. 16900 - 16909
(2020/11/30)
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- Efficient synthesis of esters through oxone-catalyzed dehydrogenation of carboxylic acids and alcohols
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Since esters are important organic synthesis intermediates, an environmentally friendly oxone catalyzed-esterification of carboxylic acids with alcohols has been developed. A series of carboxylic acid esters are obtained in high yield. This strategy requires mild reaction conditions, providing an attractive alternative for the construction of valuable carbonyl esters. Electron-rich and electron-deficient groups are compatible with the standard conditions and a variety of substrates are demonstrated. Moreover, the reaction could easily be adapted to typical prodrugs, drugs and gram-scale synthesis.
- Hou, Fei,Wang, Xi-Cun,Quan, Zheng-Jun
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supporting information
p. 9472 - 9476
(2019/01/03)
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- NOVEL SINGLE STEP ESTERIFICATION PROCESS OF ALDEHYDES USING A HETEROGENEOUS CATALYST
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The present invention relates to a novel simple, efficient and single-step process for esterification of aldehydes using a heterogeneous catalyst with high yields. More particularly, the present invention relates to a novel simple, efficient and single-step process for esterification of aldehydes using Titanium superoxide with greater than 80% yields.
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Page/Page column 23
(2016/06/20)
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- Titanium superoxide-a stable recyclable heterogeneous catalyst for oxidative esterification of aldehydes with alkylarenes or alcohols using TBHP as an oxidant
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Titanium superoxide efficiently catalysed the oxidative esterification of aldehydes with alkylarenes or alcohols, under truly heterogeneous conditions, to afford the corresponding benzyl and alkyl esters in excellent yields. Mechanistic studies have established that this "one pot" direct oxidative esterification process proceeds through a radical pathway, proven by a FTIR spectral study of a titanium superoxide-aldehyde complex as well as spin trapping experiments with TEMPO. The intramolecular version of this protocol has been successfully demonstrated in the concise synthesis of 3-butylphthalide, an anti-convulsant drug.
- Dey, Soumen,Gadakh, Sunita K.,Sudalai
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p. 10631 - 10640
(2015/11/17)
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- Rational design of substituted diarylureas: A scaffold for binding to G-quadruplex motifs
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The design and synthesis of a series of urea-based nonpolycyclic aromatic ligands with alkylaminoanilino side chains as telomeric and genomic G-quadruplex DNA interacting agents are described. Their interactions with quadruplexes have been examined by means of fluorescent resonance energy transfer melting, circular dichroism, and surface plasmon resonance-based assays. These validate the design concept for such urea-based ligands and also show that they have significant selectivity over duplex DNA, as well as for particular G-quadruplexes. The ligand-quadruplex complexes were investigated by computational molecular modeling, providing further information on structure-activity relationships. Preliminary biological studies using short-term cell growth inhibition assays show that some of the ligands have cancer cell selectivity, although they appear to have low potency for intracellular telomeric G-quadruplex structures, suggesting that their cellular targets may be other, possibly oncogene-related quadruplexes.
- Drewe, William C.,Nanjunda, Rupesh,Gunaratnam, Mekala,Beltran, Monica,Parkinson, Gary N.,Reszka, Anthony P.,Wilson, W. David,Neidle, Stephen
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supporting information; experimental part
p. 7751 - 7767
(2009/12/07)
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- UREYLENE DERIVATIVES
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The invention concerns compounds of Formula (I) or a salt, solvate or pro-drug thereof. The compounds may be used in therapy, particularly anti-cancer therapy.
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Page/Page column 48
(2008/12/04)
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- Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines
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1-Isoquinolinylguanidines were previously disclosed as potent and selective inhibitors of urokinase-type plasminogen activator (uPA). Further investigation of this template has revealed that incorporation of a 7-sulfonamide group furnishes a new series of potent and highly selective uPA inhibitors. Potency and selectivity can be achieved with sulfonamides derived from a variety of amines and is further enhanced by the incorporation of sulfonamides derived from amino acids. The binding mode of these 1-isoquinolinylguanidines has been investigated by X-ray cocrystallization studies. uPA inhibitor 26 was selected for further evaluation based on its excellent enzyme potency (Ki 10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin). In vitro, compound 26 is able to inhibit exogenous uPA in human chronic wound fluid (IC50 = 0.89 μM). In vivo, in a porcine acute excisional wound model, following topical delivery, compound 26 is able to penetrate into pig wounds and inhibit exogenous uPA activity with no adverse effect on wound healing parameters. On the basis of this profile, compound 26 (UK-371,804) was selected as a candidate for further preclinical evaluation for the treatment of chronic dermal ulcers.
- Fish, Paul V.,Barber, Christopher G.,Brown, David G.,Butt, Richard,Collis, Michael G.,Dickinson, Roger P.,Henry, Brian T.,Horne, Valerie A.,Huggins, John P.,King, Elizabeth,O'Gara, Margaret,McCleverty, Dawn,McIntosh, Fraser,Phillips, Christopher,Webster, Robert
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p. 2341 - 2351
(2008/02/03)
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- New selenyl linker for solid-phase synthesis of dehydropeptides
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A novel linker possessing selenocyanate and masked carboxylic acid was developed for the solid-phase synthesis of dehydropeptides. This linker was used to demonstrate the synthesis of the model compound of RGD-conjugated dehydropeptide.
- Nakamura, Kazuhiko,Ohnishi, Yuki,Horikawa, Eiji,Konakahara, Takeo,Kodaka, Masato,Okuno, Hiroaki
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p. 5445 - 5448
(2007/10/03)
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- Isoquinolines
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Isoquinolinylguanidine compounds of formula (I): STR1 wherein the substituents are as defined herein, and salts thereof, are disclosed as urokinase inhibitors.
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- α,α-difluorophosphonomethyl azobenzene derivatives as photoregulated phosphoamino acid analogs. 1. Design and synthesis
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A series of novel, photoregulated phosphoamino acid analogs based on an azobenzene core bearing an α,α-difluoromethylphosphonate as a hydrolytically stable phosphate isostere have been prepared with N-Fmoc protection for use in peptide synthesis. Classes of reagents analogous to both phosphotyrosine and phosphoserine/threonine were prepared by a common route employing a nitrosoarene/aniline condensation to form the azo linkage and the Cu(I)-promoted coupling of an iodoarene with (diethylphosphono)difluoromethyl cadmium bromide (Burton's method) to introduce the phosphonate moiety.
- Park, Seung Bum,Standaert, Robert F.
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p. 6557 - 6560
(2007/10/03)
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- METHOD OF INDUCING CHOLECYSTOKININ AGONIST ACTIVITY USING 1,4-BENZODIAZEPINE COMPOUNDS
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A method of inducing a Cholescystokinin-A receptor agonist response in a mammal by administering a compound of formula (I), STR1 where R 1 is C 1-C 6 alkyl, C 3-6 cycloalkyl, phenyl, or substituted phenyl; R 2 is C 3-6 alkyl, C 3-6 cycloalkyl, C 3-6 alkenyl, benzyl, phenylC 1-3 alkyl or substituted phenyl; or NR 1 R 2 together form 1,2,3,4-tetrahydroquinoline or benzazepine mono-, di-, or trisubstituted independently with C 1-6 alkyl, C 1-6 alkoxy or halogen substituents; n is an integer selected from the grouping consisting of 0, 1,2 or 3; p is the integer 0 or 1; q is the integer 0 or 1; r is the integer 0 or 1, provided that when q is 0 then r is 0; R 3, R 4, R 5 and R 8 are selected from a variety of substituents; X is nitrogen, nitroso or R 8 ; m is an integer selected from the group consisting of 0, 1, 2 or 3; Y and Z are hydrogen or halogen, novel intermediates, a pharmaceutical composition for treating obesity, gall bladder stasis, disorders of pancreatic secretion, methods for such treatment and processes for preparing compounds of formula (I).
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- CCK OR GASTRIN MODULATING 5-HETEROCYCLIC-1, 5 BENZODIAZEPINES
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Compounds of general formula (I) and physiologically salts thereof, processes for their preparation and their use as modulators of the effects of gastrin and CCK.
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- A Simple, Powerful, and Efficient Method for Transesterification
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Aromatic and α,β-unsaturated methyl esters undergo efficient transesterification at ambient temperature or below with primary, secondary, or (particularly) tertiary alcohols in the presence of butyl-lithium in tetrahydrofuran solution.
- Meth-Cohn, Otto
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p. 695 - 697
(2007/10/02)
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