Metal-free intramolecular amination: one-pot tandem synthesis of 3-substituted 4-quinolones.

abstract：:We propose to minimize the sampling time for high-throughput measurements of powder X-ray diffraction (XRD) and X-ray absorption fine structure (XAFS) in synchrotron radiation. The conventional synchrotron radiation powder X-ray diffraction method requires filling of a capillary tube, but a structure-refining diffract...

journal_title：ACS combinatorial science

authors： Fujimoto K,Aimi A,Maruyama S

更新日期：2020-12-14 00:00:00

abstract：:One-pot and efficient syntheses of structurally diverse isoquinolin-3-ones and isoquinolin-3-one-based benzo-1,4-diazepin-2,5-diones have been developed. The notable features of the process include the Ugi condensation of monomasked phthalaldehydes with amines, carboxylic acids, and isonitriles, followed by HClO4-medi...

journal_title：ACS combinatorial science

authors： Che C,Li S,Yu Z,Li F,Xin S,Zhou L,Lin S,Yang Z

更新日期：2013-04-08 00:00:00

abstract：:When isolating binders from yeast displayed combinatorial libraries, a soluble, recombinantly expressed form of the target protein is typically utilized. As an alternative, we describe the use of target proteins displayed as surface fusions on magnetized yeast cells. In our strategy, the target protein is coexpressed ...

journal_title：ACS combinatorial science

authors： Bacon K,Burroughs M,Blain A,Menegatti S,Rao BM

更新日期：2019-12-09 00:00:00

abstract：:A three-component reaction of a 2-aminoazine, a 2-oxoaldehyde, and a cyclic 1,3-dicarbonyl compound providing access toward a novel class of imidazo[1,2-a]azine derivatives was developed and studied. The scope of the process was thoroughly explored under three different reaction conditions resulting in the generation ...

journal_title：ACS combinatorial science

authors： Peshkov VA,Peshkov AA,Pereshivko OP,Van Hecke K,Zamigaylo LL,Van der Eycken EV,Gorobets NY

更新日期：2014-10-13 00:00:00

abstract：:Solid-phase synthetic strategies toward the generation of libraries of biologically relevant molecules were developed using olefin cross-metathesis as a key step. It is remarkably the formal alkane metathesis based on a one-pot, microwave-assisted, ruthenium-catalyzed cross-metathesis and reduction to obtain Csp3-Csp3...

journal_title：ACS combinatorial science

authors： Méndez L,Mata EG

更新日期：2015-02-09 00:00:00

abstract：:Functionalized chromenes have been synthesized via highly selective metal-free domino reactions from ketones and phenols. 2H-Chromenes, 4H-chromenes, spiran and benzocyclopentane can be respectively prepared starting from the corresponding cyclic ketones, aryl methyl ketones, acetone, and 3-pentanone. ...

journal_title：ACS combinatorial science

authors： Xue WJ,Li Q,Gao FF,Zhu YP,Wang JG,Zhang W,Wu AX

更新日期：2012-08-13 00:00:00

abstract：:The present investigation reports an easy access to a library of novel spiro-oxindole-pyrrolizine or pyrrolo[1,2-c]thiazole fused coumarin hybrid heterocycles through a one-pot sequential four-component reactions of 2,2-dimethyl-1,3-dioxane-4,6-dione, salicylaldehydes, isatins, and cyclic α-amino acids under ultrasoun...

journal_title：ACS combinatorial science

authors： Kanchithalaivan S,Sumesh RV,Kumar RR

更新日期：2014-10-13 00:00:00

abstract：:An unprecedented three-component C(sp(3))-H functionalization of 2-alkylazaarenes with aryl aldehydes and 4-hydroxycoumarins was realized, providing azaarene-substituted 3-benzyl-4-hydroxycoumarins in good to excellent yields. These new target compounds displayed broad-spectrum antibacterial activities, providing a ne...

journal_title：ACS combinatorial science

authors： Dong H,Xu L,Li SS,Wang L,Shao CL,Xiao J

更新日期：2016-09-12 00:00:00

abstract：:A fast and facile synthesis of a series of 4-nitrophenyl 2-azidoethylcarbamate derivatives as activated urea building blocks was developed. The N-Fmoc-protected 2-aminoethyl mesylates derived from various commercially available N-Fmoc-protected α-amino acids, including those having functionalized side chains with acid...

journal_title：ACS combinatorial science

authors： Chen YY,Chang LT,Chen HW,Yang CY,Hsin LW

更新日期：2017-03-13 00:00:00

abstract：:A set of chemically engineered extracts enriched in compounds including N-N and N-O fragments in their structures was prepared. Bromodomain binding screening and bioguided fractionation led to the identification of one oxime hit that interacts with TcBDF3 with affinity in the submicromolar range and that shows interes...

journal_title：ACS combinatorial science

authors： Ramallo IA,Alonso VL,Rua F,Serra E,Furlan RLE

更新日期：2018-04-09 00:00:00

abstract：:A potentiometric Pb(II)-selective sensor was fabricated by a combinatorial screening of electrically conducting polysulfoaminoanthraquinone (PSA) nanoparticles as a solid ionophore, ion exchangers (oleic acid (OA) and NaTPB), plasticizers in a polyvinyl chloride (PVC) matrix, membrane thickness, inner filling ion spec...

journal_title：ACS combinatorial science

authors： Huang MR,Ding YB,Li XG

更新日期：2014-03-10 00:00:00

abstract：:A novel parallel medicinal chemistry (PMC)-enabled synthesis of 1H-pyrazolo[3,4-d]pyrimidines employing condensation of easily accessible N-pyrazolylamides and nitriles has been developed. The presented studies describe singleton and library enablements that allowed rapid generation of molecular diversity to examine C...

journal_title：ACS combinatorial science

authors： Shah AA,Chenard LK,Tucker JW,Helal CJ

更新日期：2017-11-13 00:00:00

abstract：:Protein-protein interactions are generally challenging to target by small molecules. To address the challenge, we have used a multidisciplinary approach to identify small-molecule disruptors of protein-protein interactions that are mediated by SUMO (small ubiquitin-like modifier) proteins. SUMO modifications have emer...

journal_title：ACS combinatorial science

authors： Alontaga AY,Li Y,Chen CH,Ma CT,Malany S,Key DE,Sergienko E,Sun Q,Whipple DA,Matharu DS,Li B,Vega R,Li YJ,Schoenen FJ,Blagg BS,Chung TD,Chen Y

更新日期：2015-04-13 00:00:00

abstract：:In this research, MgAl-CO32- nanolayered double hydroxide (NLDH) was synthesized through a facile coprecipitation method, followed by a hydrothermal treatment. The prepared NLDHs were used as a hydrophilic nanofiller for improving the performance of the PVDF-based ultrafiltration membranes. The main objective of this ...

journal_title：ACS combinatorial science

authors： Arefi-Oskoui S,Khataee A,Vatanpour V

更新日期：2017-07-10 00:00:00

abstract：:Peptides are still difficult to synthesize when they contain sterically hindered amino acids, such as α,α-disubstituted amino acids and N-substituted amino acids. In this study, solid-phase syntheses of oligopeptides containing multiple α-aminoisobutyric acid (Aib) residues were performed in high yields by using a non...

journal_title：ACS combinatorial science

authors： Hara RI,Mitsuhashi Y,Saito K,Maeda Y,Wada T

更新日期：2018-03-12 00:00:00

abstract：:For a future structure-activity relationship (SAR) study, a library of desketoraloxifene analogues has been prepared by parallel synthesis using iodocyclization and subsequent palladium-catalyzed coupling reactions. Points of desketoraloxifene diversification involve the two phenolic hydroxyl groups and the aliphatic ...

journal_title：ACS combinatorial science

authors： Cho CH,Jung DI,Neuenswander B,Larock RC

更新日期：2011-09-12 00:00:00

abstract：:Fourteen (hetero-)(arylidene)arylhydrazide derivatives (ABH1-ABH14) were synthesized, and their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE) were evaluated. Compound ABH5 most potently inhibited MAO-B with an IC50 value of 0.025 ± 0.0019 μM; ABH2 and ABH3 exhibited high IC50 ...

journal_title：ACS combinatorial science

authors： Palakkathondi A,Oh JM,Dev S,Rangarajan TM,Kaipakasseri S,Kavully FS,Gambacorta N,Nicolotti O,Kim H,Mathew B

更新日期：2020-11-09 00:00:00

abstract：:An efficient and straightforward synthetic protocol has been developed for the diversity-oriented synthesis of highly functionalized piperidines containing a Meldrum's acid moiety via pseudo five-component reaction between aromatic aldehydes, ammonium acetate, substituted β-nitrostyrenes and Meldrum's acid for the gen...

journal_title：ACS combinatorial science

authors： Li Y,Xue Z,Ye W,Liu J,Yao J,Wang C

更新日期：2014-03-10 00:00:00

abstract：:A new one-pot, three component reaction involving the use of Julia reagent, aldehyde, and sodium azide was developed for the efficient synthesis of N-unsubstituted 1,2,3-triazoles. This reaction could be carried out under mild reaction conditions without any precaution, and broad scope of substrates, both respect to J...

journal_title：ACS combinatorial science

authors： Chai H,Guo R,Yin W,Cheng L,Liu R,Chu C

更新日期：2015-03-09 00:00:00

abstract：:Metal-organic frameworks (MOFs) are nanoporous materials with exceptional host-guest properties poised for groundbreaking innovations in gas separation applications according to high-throughput (HT) screening data. However, MOF structural libraries are nearly infinite in practice and so statistical and information tec...

journal_title：ACS combinatorial science

authors： Fernandez M,Barnard AS

更新日期：2016-05-09 00:00:00

abstract：:We report the parallel synthesis of a series of novel 4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-3-ium chloride salts, which are analogs to cationic anthraquinones. Three synthetic protocols were examined leading to a convenient and facile library synthesis of the cationic anthraquinone analogs that contain...

journal_title：ACS combinatorial science

authors： Fosso MY,Chan KY,Gregory R,Chang CW

更新日期：2012-03-12 00:00:00

abstract：:A build/couple/pair strategy for the synthesis of complex and densely functionalized small molecules is presented. The strategy relies on synthetically tractable building blocks (build), that is, diversely substituted hydrazides, α-hydroxy aldehydes, and boronic acids, which undergo Petasis 3-component reactions (coup...

journal_title：ACS combinatorial science

authors： Flagstad T,Hansen MR,Le Quement ST,Givskov M,Nielsen TE

更新日期：2015-01-12 00:00:00

abstract：:An efficient discovery strategy by combining diversity-oriented synthesis and converging cellular screening is described. By a three-round screening process, we identified novel tricyclic pyrido[2,3-b][1,4]benzothiazepines showing potent inhibitory activity against paclitaxel-resistant cell line H460TaxR (EC50 < 1.0 μ...

journal_title：ACS combinatorial science

authors： Xiang J,Zhang Z,Mu Y,Xu X,Guo S,Liu Y,Russo DP,Zhu H,Yan B,Bai X

更新日期：2016-05-09 00:00:00

abstract：:This work presents the first use of yeast-displayed protein targets for screening mRNA-display libraries of cyclic and linear peptides. The WW domains of Yes-Associated Protein 1 (WW-YAP) and mitochondrial import receptor subunit TOM22 were adopted as protein targets. Yeast cells displaying WW-YAP or TOM22 were magnet...

journal_title：ACS combinatorial science

authors： Bacon K,Bowen J,Reese H,Rao BM,Menegatti S

更新日期：2020-12-14 00:00:00

abstract：:The possibility of band gap engineering in graphene opens countless new opportunities for application in nanoelectronics. In this work, the energy gaps of 622 computationally optimized graphene nanoflakes were mapped to topological autocorrelation vectors using machine learning techniques. Machine learning modeling re...

journal_title：ACS combinatorial science

authors： Fernandez M,Abreu JI,Shi H,Barnard AS

更新日期：2016-11-14 00:00:00

abstract：:Parallel solution-phase synthesis of combinatorial libraries of dihydroindenoisoquinolines employing a sequential Cu(I)/Pd(0)-catalyzed multicomponent coupling and annulation protocol was realized. The scope and limitations of the protocol with respect to the substitution pattern in the aryl ring of the indene core, a...

journal_title：ACS combinatorial science

authors： Kumar S,Painter TO,Pal BK,Neuenswander B,Malinakova HC

更新日期：2011-09-12 00:00:00

abstract：:A combination of flow and batch chemistries has been successfully applied to the assembly of a series of trisubstituted drug-like pyrrolidines. This study demonstrates the efficient preparation of a focused library of these pharmaceutically important structures using microreactor technologies, as well as classical par...

journal_title：ACS combinatorial science

authors： Baumann M,Baxendale IR,Kuratli C,Ley SV,Martin RE,Schneider J

更新日期：2011-07-11 00:00:00

abstract：:Dispiro-pyrrolidino/pyrrolizidino fused oxindoles/acenaphthoquinones have been derived from andrographolide via azomethine ylide cycloaddition to the conjugated double-bond under microwave (MW) irradiation. The reactions are chemo-, stereo-, and regioselective in nature. Change in amino acid from sarcosine/N-benzyl gl...

journal_title：ACS combinatorial science

authors： Hazra A,Bharitkar YP,Chakraborty D,Mondal SK,Singal N,Mondal S,Maity A,Paira R,Banerjee S,Mondal NB

更新日期：2013-01-14 00:00:00

abstract：:On the basis of computational design, a focused one-bead one-compound library has been prepared on microparticle-encoded PEGA1900 beads consisting of small tripeptides with a triazole-capped N-terminal. The library was screened towards a double point-mutated version of the human FKBP12 protein, known as the destabiliz...

journal_title：ACS combinatorial science

authors： Madsen D,Jørgensen FP,Palmer D,Roux ME,Olsen JV,Bols M,Schoffelen S,Diness F,Meldal M

更新日期：2020-03-09 00:00:00

abstract：:A microgradient-heater (MGH) was developed, and its feasibility as a tool for high-throughput materials science experimentation was tested. The MGH is derived from microhot plate (MHP) systems and allows combinatorial thermal processing on the micronano scale. The temperature gradient is adjustable by the substrate ma...

journal_title：ACS combinatorial science

authors： Meyer R,Hamann S,Ehmann M,Thienhaus S,Jaeger S,Thiede T,Devi A,Fischer RA,Ludwig A

更新日期：2012-10-08 00:00:00