One-pot multicomponent synthesis of highly functionalized piperidines from substituted β-nitrostyrenes, Meldrum's acid, aromatic aldehydes, and ammonium acetate.

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：:A one-pot parallel synthesis of N(1)-aryl-N(2)-alkyl-substituted oxamides with 2,2,2-trifluoroethyl chlorooxoacetate was developed. The synthesis of a library of 45 oxamides revealed higher efficiency of this reagent over the known ethyl chlorooxoacetate. The reagent was successfully used to prepare the known oxamide-...

journal_title：ACS combinatorial science

authors： Bogolubsky AV,Moroz YS,Mykhailiuk PK,Pipko SE,Zhemera AV,Konovets AI,Stepaniuk OO,Myronchuk IS,Dmytriv YV,Doroschuk RA,Zaporozhets OA,Tolmachev A

更新日期：2015-10-12 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：:Ultrasound-assisted synthesis of benzimidazo[2,1-b]quinazolin-1(1H)-ones was achieved via piperidine-catalyzed three-component reaction of 2-aminobenzimidazoles, an aromatic aldehyde, and 1,3-dione in aqueous isopropanol. This mechanism was first suspected following our identification of unusual reaction intermediates...

journal_title：ACS combinatorial science

authors： Chen LH,Chung TW,Narhe BD,Sun CM

更新日期：2016-03-14 00:00:00

abstract：:A combination of MACOS scale-out and ROMP-derived oligomeric triazole phosphates (OTP(n)) have been successfully utilized for the preparation of a 106-member library of triazole containing benzothiaoxazepine-1,1-dioxides. This report demonstrates the utilization of a suite of soluble OTP(n) reagents for facile (triazo...

journal_title：ACS combinatorial science

authors： Faisal S,Ullah F,Maity PK,Rolfe A,Samarakoon TB,Porubsky P,Neuenswander B,Lushington GH,Basha FZ,Organ MG,Hanson PR

更新日期：2012-04-09 00:00:00

abstract：:This paper describes the synthesis of a 300 member library of 3,5-substituted enones. The synthesis starts with 6 different bromoenones that are accessed from the corresponding 1,3 diones. These bromides are then diversified by Suzuki coupling with a variety of aromatic and vinyl boronic acids. Additionally a small se...

journal_title：ACS combinatorial science

authors： Khalaf J,Estrella-Jimenez ME,Shashack MJ,Phatak SS,Zhang S,Gilbertson SR

更新日期：2011-07-11 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：:Competition-enhanced ligand screening (CompELS) was employed to rapidly screen through large DNA libraries to identify single-stranded, oligonucleotide-based ligands called aptamers that bind to a nonbiological target. This previously unreported aptamer screening approach involves the repeated introduction of unenrich...

journal_title：ACS combinatorial science

authors： Tapp MJN,Slocik JM,Dennis PB,Naik RR,Milam VT

更新日期：2018-10-08 00:00:00

abstract：:A one-pot, three-component synthesis of benzimidazole-linked thiazolidines from 2-cyanomethyl benzimidazole, iso-, isothio-, or isoselenocyanates and 1,2-dichloroethane is reported. Isolation of the key intermediate formed during the course of the reaction validates its mechanistic pathway. Under the same reaction con...

journal_title：ACS combinatorial science

authors： Lu HY,Barve IJ,Selvaraju M,Sun CM

更新日期：2020-01-13 00:00:00

abstract：:The exploration of new alloys with desirable properties has been a long-standing challenge in materials science because of the complex relationship between composition and microstructure. In this Research Article, we demonstrate a combinatorial strategy for the exploration of composition dependence of microstructure. ...

journal_title：ACS combinatorial science

authors： Li Y,Jensen KE,Liu Y,Liu J,Gong P,Scanley BE,Broadbridge CC,Schroers J

更新日期：2016-10-10 00:00:00

abstract：:The development of a scanning reactor for planar catalysts is presented here. With respect to other existing models, this reactor is able to scan catalysts even with low turnover frequencies with a minimum sensed circular area of approximately 6 mm in diameter. The downstream gas analysis is performed with a quaprupol...

journal_title：ACS combinatorial science

authors： Marelli M,Nemenyi A,Dal Santo V,Psaro R,Ostinelli L,Monticelli D,Dossi C,Recchia S

更新日期：2016-01-11 00:00:00

abstract：:Electromanipulation and electrical characterization of cancerous cells is becoming a topic of high interest as the results reported to date demonstrate a good differentiation among various types of cells from an electrical viewpoint. Dielectrophoresis and broadband dielectric spectroscopy are complementary tools for s...

journal_title：ACS combinatorial science

authors： Turcan I,Olariu MA

更新日期：2020-11-09 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：: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：:Thirteen 5-hetarylaminopyrazoles were synthesized in 62-93% yield through the arylation of 1-isopropyl- and 1-phenyl-5-aminopyrazoles with electrophilic hetarylhalides under optimized conditions. Condensation of 5-hetarylaminopyrazoles with carbonyl compounds facilitated by AcOH or Me(3)SiCl furnished 23 pyrazolo[3,4-...

journal_title：ACS combinatorial science

authors： Ryabukhin SV,Granat DS,Plaskon AS,Shivanyuk AN,Tolmachev AA,Volovenko YM

更新日期：2012-08-13 00:00:00

abstract：:In view of the variety and complexity of thermoelectric (TE) material systems, combinatorial approaches to materials development come to the fore for identifying new promising compounds. The success of this approach is related to the availability and reliability of high-throughput characterization methods for identify...

journal_title：ACS combinatorial science

authors： Ziolkowski P,Wambach M,Ludwig A,Mueller E

更新日期：2018-01-08 00:00:00

abstract：:An efficient method is described for the solid-supported synthesis of imidazo[4,5-b]pyridines and imidazo[4,5-c]pyridines from 2,4-dichloro-3-nitropyridine. The key pyridine building block was reacted with polymer-supported amines, followed by replacement of the second chlorine with amines, nitro group reduction, and ...

journal_title：ACS combinatorial science

authors： Lemrová B,Smyslová P,Popa I,Oždian T,Zajdel P,Soural M

更新日期：2014-10-13 00:00:00

abstract：:High-throughput experimentation provides efficient mapping of composition-property relationships, and its implementation for the discovery of optical materials enables advancements in solar energy and other technologies. In a high throughput pipeline, automated data processing algorithms are often required to match ex...

journal_title：ACS combinatorial science

authors： Suram SK,Newhouse PF,Gregoire JM

更新日期：2016-11-14 00:00:00

abstract：:Preparative RP-LCMS is widely used to purify compounds from crude reaction mixtures in drug discovery today. Method development for preparative Liquid Chromatography-Mass Spectrometry (LCMS) consists of finding the right balance between speed and quality, often leading to the use of fast generic gradients (5-95% organ...

journal_title：ACS combinatorial science

authors： Koza P,Gonnot V,Pelleter J

更新日期：2012-04-09 00:00:00

abstract：:Acetylenic tertiary alcohols are well-known to be compounds that are biologically more stable than their corresponding secondary alcohols. The linkage of an acetylenic compound to a polymer support and further introduction of molecular diversity was found to be an interesting way to generate libraries of hydroxy acety...

journal_title：ACS combinatorial science

authors： Talbot A,Maltais R,Poirier D

更新日期：2012-06-11 00:00:00

abstract：:Disulfide exchange screening is a method for evaluating the binding of small molecule fragments to proteins that have at least one accessible cysteine. While operationally simple, it does require a large library of small fragment molecules bearing disulfide-containing side chains. These specialized fragments are not a...

journal_title：ACS combinatorial science

authors： Burlingame MA,Tom CT,Renslo AR

更新日期：2011-05-09 00:00:00

abstract：:We have implemented an aldol-based "build/couple/pair" (B/C/P) strategy for the synthesis of stereochemically diverse 8-membered lactam and sultam scaffolds via S(N)Ar cycloetherification. Each scaffold contains two handles, an amine and aryl bromide, for solid-phase diversification via N-capping and Pd-mediated cross...

journal_title：ACS combinatorial science

authors： Gerard B,Duvall JR,Lowe JT,Murillo T,Wei J,Akella LB,Marcaurelle LA

更新日期：2011-07-11 00:00:00

abstract：:A novel three-component, two-step, one-pot nucleophilic aromatic substitution (SNAr)-intramolecular cyclization-Suzuki coupling reaction was developed for the synthesis of benzo[h][1,6]naphthyridin-2(1H)-ones (Torins). On the basis of the new efficiently convergent synthetic route, a library of Torin analogs was synth...

journal_title：ACS combinatorial science

authors： Li H,Sun W,Huang X,Lu X,Patel PR,Kim M,Orr MJ,Fisher RM,Tanaka TQ,McKew JC,Simeonov A,Sanderson PE,Zheng W,Williamson KC,Huang W

更新日期：2017-12-11 00:00:00

abstract：:A sequential single-flask multicomponent reactions is highly effective for the synthesis of 1,2-dihydroisoquinolines through amidealkylation from intermediate N-acylisoquinolinium salts under mild conditions. N-Acylisoquinolinium ions and trichloromethyl-1-(1H-indol-3-yl)isoquinoline-2(1H)-carboxylate have demonstrate...

journal_title：ACS combinatorial science

authors： Chung TW,Hung YT,Thikekar T,Paike VV,Lo FY,Tsai PH,Liang MC,Sun CM

更新日期：2015-08-10 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：: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：: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：: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：: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：: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