One-pot syntheses of isoquinolin-3-ones and benzo-1,4-diazepin-2,5-diones utilizing Ugi-4CR post-transformation strategy.

abstract：:Under the acidic conditions, substituted furans were constructed from γ-alkynyl ketones through corresponding allene intermediates in one-pot. The methodology was also tailored to a series of the Ugi reaction products for the synthesis of 6-methylpyrazin-2(1 H)-one derivatives. The current method offered significant a...

journal_title：ACS combinatorial science

authors： Lei J,Xu ZG,Tang DY,Li Y,Xu J,Li HY,Zhu J,Chen ZZ

更新日期：2018-05-14 00:00:00

abstract：:A high throughput combinatorial synthesis utilizing inkjet printing of precursor inks was used to rapidly evaluate Bi-alloying into double perovskite oxides for enhanced visible light absorption. The fast visual screening of photo image scans of the library plates identifies 4-metal oxide compositions displaying an in...

journal_title：ACS combinatorial science

authors： Newhouse PF,Zhou L,Umehara M,Boyd DA,Soedarmadji E,Haber JA,Gregoire JM

更新日期：2020-12-14 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：:Adleman's illustration of molecular computing using DNA paved the way toward an entirely new direction of computing (Adleman, L. M. Science 1994, 266, 1021). The exponential time complex combinatorial problem on a traditional computer turns out to be a separation problem involving a polynomial number of steps in DNA c...

journal_title：ACS combinatorial science

authors： Sharma D,Ramteke M

更新日期：2020-05-11 00:00:00

abstract：:An efficient, three-component strategy for the improved synthesis of multifunctionalized 6,7-dihydrobenzofuran-4(5H)-ones under microwave irradiation in ethyl alcohol within short periods has been established. The synthesized benzofuran-4(5H)-ones have been readily converted into polyfunctionalized cinnoline-4-carboxa...

journal_title：ACS combinatorial science

authors： Ma GH,Tu XJ,Ning Y,Jiang B,Tu SJ

更新日期：2014-06-09 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：:The thin film system Ti-Ni-Si was investigated using methods of combinatorial materials science. A thin film composition spread library of the system was fabricated using combinatorial magnetron sputtering. The functional properties Seebeck coefficient, electrical resistivity, and luminance were determined using high-...

journal_title：ACS combinatorial science

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

更新日期：2019-05-13 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：: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：: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：: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：: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：:Optical bandgap mapping of Nb-Ti mixed oxides anodically grown on a thin film parent metallic combinatorial library was performed via variable angle spectroscopic ellipsometry (VASE). A wide Nb-Ti compositional spread ranging from Nb-90 at.% Ti to Nb-15 at.% Ti deposited by cosputtering was used for this purpose. The ...

journal_title：ACS combinatorial science

authors： Bleckenwegner P,Mardare CC,Cobet C,Kollender JP,Hassel AW,Mardare AI

更新日期：2017-02-13 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 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：: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：: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：:Solid-phase synthesis is the method of choice for peptide preparation in both research and industrial settings. The whole synthetic process is governed by the initial functionalization of the resin. Although the literature provides several methods to determine such functionalization, the addition of an Fmoc-amino acid...

journal_title：ACS combinatorial science

authors： Al Musaimi O,Basso A,de la Torre BG,Albericio F

更新日期：2019-11-11 00:00:00

abstract：:High-throughput combinatorial methods have been useful in identifying new oxide semiconductors with the potential to be applied to solar water splitting. Most of these techniques have been limited to producing and screening oxide phases formed at temperatures below approximately 550 °C. We report the development of a ...

journal_title：ACS combinatorial science

authors： Skorupska K,Maggard PA,Eichberger R,Schwarzburg K,Shahbazi P,Zoellner B,Parkinson BA

更新日期：2015-12-14 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：: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：: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：: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：: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：:A novel and highly efficient three-component reaction of 2-alkynylbenzaldoxime, carbodiimide, with electrophile (bromine or iodine monochloride) is disclosed, which generates 1-(4-haloisoquinolin-1-yl)ureas in good yields under mild conditions. Subsequent palladium-catalyzed Suzuki-Miyaura coupling reaction is introdu...

journal_title：ACS combinatorial science

authors： Ye S,Wang H,Wu J

更新日期：2011-03-14 00:00:00

abstract：:A series of diverse polycyclic heterocycles containing spirooxindole, pyridine/thiophene, and pyrrolidine/pyrrolizidine/pyrrolothiazole rings have been synthesized through the 1,3-dipolar cycloaddition of azomethine ylides generated in situ by the condensation of dicarbonyl compounds (isatin or acenaphthenequinone) an...

journal_title：ACS combinatorial science

authors： Li J,Wang J,Xu Z,Zhu S

更新日期：2014-09-08 00:00:00

abstract：:High-throughput calculations can be applied to a large number of compounds, in order to discover new useful materials. In the present work, ternary intermetallic compounds are investigated, to find new potentially interesting materials for thermoelectric applications. The screening of stable nonmetallic compounds requ...

journal_title：ACS combinatorial science

authors： Barreteau C,Crivello JC,Joubert JM,Alleno E

更新日期：2020-12-14 00:00:00

abstract：:Retinoic acid (RA) is a key metabolite necessary for embryonic development and differentiation in vertebrates. We demonstrate the utility of genetically encoded, ligand-activatable single-chain bioluminescence probes for detecting RAs from different biological sources. We examined 13 different molecular designs to ide...

journal_title：ACS combinatorial science

authors： Kim SB,Fujii R,Nishihara R,Bose RJ,Citterio D,Suzuki K,Massoud TF,Paulmurugan R

更新日期：2019-06-10 00:00:00

abstract：:DNA-encoded synthesis is rekindling interest in combinatorial compound libraries for drug discovery and in technology for automated and quantitative library screening. Here, we disclose a microfluidic circuit that enables functional screens of DNA-encoded compound beads. The device carries out library bead distributio...

journal_title：ACS combinatorial science

authors： MacConnell AB,Price AK,Paegel BM

更新日期：2017-03-13 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