Metal-free, ionic liquid-mediated synthesis of functionalized quinolines.

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：: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：: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 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 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：:A series of LiMn1-x-yFexVyPO4 (LMFVP) nanomaterials have been synthesized using a pilot-scale continuous hydrothermal synthesis process (CHFS) and evaluated as high voltage cathodes in Li-ion batteries at a production rate of 0.25 kg h-1. The rapid synthesis and screening approach has allowed the specific capacity of ...

journal_title：ACS combinatorial science

authors： Johnson ID,Loveridge M,Bhagat R,Darr JA

更新日期：2016-11-14 00:00:00

abstract：:This is a report on the early years of combinatorial materials science and technology. High-throughput technologies (HTTs) are found in life- and materials-science laboratories. Although HTTs have long been the standard in life sciences in academia as well as in industry, HTTs in materials science have become the stan...

journal_title：ACS combinatorial science

authors： Maier WF

更新日期：2019-06-10 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：:Cr-Al-N thin film materials libraries were synthesized by combinatorial reactive high power impulse magnetron sputtering (HiPIMS). Different HiPIMS repetition frequencies and peak power densities were applied altering the ion to growth flux ratio. Moreover, time-resolved ion energy distribution functions were measured...

journal_title：ACS combinatorial science

authors： Banko L,Ries S,Grochla D,Arghavani M,Salomon S,Pfetzing-Micklich J,Kostka A,Rogalla D,Schulze J,Awakowicz P,Ludwig A

更新日期：2019-12-09 00:00:00

abstract：:A build/couple/pair (B/C/P) strategy was employed to generate a library of 7936 stereochemically diverse 12-membered macrolactams. All 8 stereoisomers of a common linear amine precursor were elaborated to form the corresponding 8 stereoisomers of two regioisomeric macrocyclic scaffolds via head-to-tail cyclization. Su...

journal_title：ACS combinatorial science

authors： Fitzgerald ME,Mulrooney CA,Duvall JR,Wei J,Suh BC,Akella LB,Vrcic A,Marcaurelle LA

更新日期：2012-02-13 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：:Polymer-supported N-(2-oxo-ethyl)-derivatized Ser/Thr/Cys-containing dipeptides were synthesized and subjected to acid-mediated tandem N-acylium ion cyclization-nucleophilic addition to yield tetrahydro-2H-oxazolo[3,2-a]pyrazin-5(3H)-ones. The reaction conditions and building-block combinations for stereoselective syn...

journal_title：ACS combinatorial science

authors： La Venia A,Dolenský B,Krchňák V

更新日期：2013-03-11 00:00:00

abstract：:We report the first example of venting-while-heating microwave-assisted synthesis of a small library of 3-arylthioindoles. Compounds were prepared in excellent isolated yields (90-98%) within 4 min in a closed vessel by treating indoles with disulfides in the presence of sodium hydride in anhydrous N,N-dimethylformami...

journal_title：ACS combinatorial science

authors： La Regina G,Gatti V,Famiglini V,Piscitelli F,Silvestri R

更新日期：2012-04-09 00:00:00

abstract：:A library of functionalized 3-(α-styryl)-benzo[b]thiophenes, endowed with a high level of molecular diversity, was efficiently synthesized by applying a synthetic sequence that allowed introduction of various substituents on aromatic A, B, and C-rings. The strategy developed involves the synthesis of 3-bromobenzo[b]th...

journal_title：ACS combinatorial science

authors： Tréguier B,Lawson M,Bernadat G,Bignon J,Dubois J,Brion JD,Alami M,Hamze A

更新日期：2014-12-08 00:00:00

abstract：:A combinatorial library having 66 different ternary compositions of Pd-Ir-Ce was prepared via the impregnation method to find the optimum ternary composition with the highest performance toward oxygen reduction reaction (ORR) in acid media. Its performance in ORR activity of the combinatorial array was evaluated throu...

journal_title：ACS combinatorial science

authors： Park SH,Choi CH,Koh JK,Pak C,Jin SA,Woo SI

更新日期：2013-11-11 00:00:00

abstract：:A sequential one-pot, two-step, three-component reaction for efficient synthesis of spiro-substituted 1,3-thiazine library has been developed. The syntheses were achieved by reacting cyanoacetamide with isothiocyanate derivatives to give rise to 2-cyano-3-mercaptoacrylamides, which are trapped in situ by various cyclo...

journal_title：ACS combinatorial science

authors： Zhuang QY,Wang X,Gao Y,Shi F,Jiang B,Tu SJ

更新日期：2011-01-10 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：:Unfunctionalized alkylbiphenyls were fabricated by a parallel and combinatorial synthesis using pentaerythritol as a tetrapodal soluble support for a sulfonate-based traceless multifunctional linker system. Nickel N-heterocyclic carbene-catalyzed reactions of pentaerythritol tetrakis(biphenylsulfonate)s with primary a...

journal_title：ACS combinatorial science

authors： Kim WK,Jang JH,Jo H,Park K

更新日期：2014-05-12 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：: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：: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：: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：: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：:We have achieved an efficient solution-phase parallel synthesis of a library of natural piper-amide-like compounds from the bifunctional β-phosphono-N-hydroxy-succinimidyl ester intermediate. The primary important feature in our study is the construction of natural-product-like molecules through the adaptation of soph...

journal_title：ACS combinatorial science

authors： Kim S,Lim C,Lee S,Lee S,Cho H,Lee JY,Shim DS,Park HD,Kim S

更新日期：2013-04-08 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：:The Au-Al alloy system was investigated via a combinatorial thin film sputtering method for its potential as a plasmonic material. Au xAl1- x combinatorial libraries were cosputtered from Au and Al elemental targets and the composition, phase, and dielectric function of a ∼350 nm film was determined using energy dispe...

journal_title：ACS combinatorial science

authors： Collette R,Wu Y,Olafsson A,Camden JP,Rack PD

更新日期：2018-11-12 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：: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：: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：: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