- Porous polymeric ligand promoted copper-catalyzed C-N coupling of (hetero)aryl chlorides under visible-light irradiation
-
A porous polymeric ligand (PPL) has been synthesized and complexed with copper to generate a heterogeneous catalyst (Cu@PPL) that has facilitated the efficient C-N coupling with various (hetero)aryl chlorides under mild conditions of visible-light irradiation at 80 °C (58 examples, up to 99% yields). This method could be applied to both aqueous ammonia and substituted amines, and is compatible to a variety of functional groups and heterocycles, as well as allows tandem C-N couplings with conjunctive dihalides. Furthermore, the heterogeneous characteristic of Cu@PPL has enabled a straightforward catalyst separation in multiple times of recycling with negligible catalytic efficiency loss by simple filtration, affording reaction mixtures containing less than 1 ppm of Cu residue. [Figure not available: see fulltext.]
- Wang, Erfei,Chen, Kaixuan,Chen, Yinan,Zhang, Jiawei,Lin, Xinrong,Chen, Mao
-
-
- Innovative Multipodal Ligands Derived from Tr?ger's Bases for the Sensitization of Lanthanide(III) Luminescence
-
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
-
p. 16900 - 16909
(2020/11/30)
-
- Carbamic acid 2-trimethylsilylethyl ester as a new ammonia equivalent for palladium-catalyzed amination of aryl halides
-
Carbamic acid 2-trimethylsilylethyl ester (Teoc-NH2) serves as an ammonia equivalent in the palladium-catalyzed amination of aryl bromides and aryl chlorides. Anilines with sensitive functional groups can be readily prepared using these amine derivatives.
- Mullick, Dibakar,Anjanappa, Prakash,Selvakumar, Kumaravel,Ruckmani, Kandasamy,Sivakumar, Manickam
-
supporting information; experimental part
p. 5984 - 5987
(2010/11/21)
-
- 2-(Trimethylsilyl)ethanesulfonyl amide as a new ammonia equivalent for palladium-catalyzed amination of aryl halides
-
2-(Trimethylsilyl)ethanesulfonyl amide (SES-NH2) is an ammonia equivalent for the palladium-catalyzed amination of aryl bromides and aryl chlorides. Using these amine derivatives, it has been observed that anilines and anilines with sensitive functional groups can be readily prepared.
- Anjanappa, Prakash,Mullick, Dibakar,Selvakumar, Kumaravel,Sivakumar, Manickam
-
p. 4585 - 4587
(2008/09/21)
-
- Rational design of substituted diarylureas: A scaffold for binding to G-quadruplex motifs
-
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
-
supporting information; experimental part
p. 7751 - 7767
(2009/12/07)
-
- UREYLENE DERIVATIVES
-
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.
- -
-
Page/Page column 48-49
(2008/12/04)
-
- Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines
-
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
-
p. 2341 - 2351
(2008/02/03)
-
- Composition for the treatment of damaged tissue
-
A pharmaceutical for use in damaged tissue, such as wound, treatment (e.g. healing) is described. The pharmaceutical comprising a composition which comprises: (a) a growth factor; and (b) an inhibitor agent; and optionally (c) a pharmaceutically acceptable carrier, diluent or excipient; wherein the inhibitor agent can inhibit the action of at least one specific adverse protein (e.g. a specific protease) that is upregulated in a damaged tissue, such as a wound, environment.
- -
-
-
- New selenyl linker for solid-phase synthesis of dehydropeptides
-
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
-
p. 5445 - 5448
(2007/10/03)
-
- Palladium-Catalyzed Animation of Aryl Halides on Solid Support
-
(Matrix Presented) The first examples of the Pd(0)-catalyzed amination of aryl halides using Rink-resins as nitrogen source are described. Pd2dba3/BINAP/NaO-t-Bu was found to be the most efficient catalyst/base system, while a solvent mixture of dioxane and tert-butyl alcohol was shown to enhance the selectivity toward the desired monoarylation. Moderate to good yields and excellent purities of the amination products were found with electron-poor aryl halides, while electon-rich aryl halides failed to react under these conditions.
- Weigand, Klaus,Pelka, Sylvie
-
p. 4689 - 4692
(2007/10/03)
-
- Isoquinolines
-
Isoquinolinylguanidine compounds of formula (I): STR1 wherein the substituents are as defined herein, and salts thereof, are disclosed as urokinase inhibitors.
- -
-
-
- α,α-difluorophosphonomethyl azobenzene derivatives as photoregulated phosphoamino acid analogs. 1. Design and synthesis
-
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.
-
p. 6557 - 6560
(2007/10/03)
-
- METHOD OF INDUCING CHOLECYSTOKININ AGONIST ACTIVITY USING 1,4-BENZODIAZEPINE COMPOUNDS
-
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).
- -
-
-
- CCK OR GASTRIN MODULATING 5-HETEROCYCLIC-1, 5 BENZODIAZEPINES
-
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.
- -
-
-