- Efficient and expeditious chemoselective BOC protection of amines in catalyst and solvent-free media
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A green and eco-friendly route for the almost quantitative BOC protection of a large variety of aliphatic and aromatic amines, amino acids, and amino alcohols is reported in catalyst and solvent-free media under mild reaction conditions. The products were confirmed by 1H, 13C NMR, IR spectroscopy, and in some cases, elemental analysis. This protocol does not require any water quenches, solvent separations, and purification steps, such as recrystallization and column chromatography.
- Viswanadham, Balaga,Mahomed, Abdul S.,Friedrich, Holger B.,Singh, Sooboo
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p. 1355 - 1363
(2017/02/15)
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- FUSED THIAZOLOPYRIMIDINE DERIVATIVES AS MNKS INHIBITORS
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The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably, Alzheimer's disease.
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Page/Page column 65; 66
(2017/06/12)
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- An efficient one-pot oxidative esterification of aldehydes to carboxylic esters using B(C6F5)3-TBHP
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A simple and efficient protocol for oxidative esterification of diverse aldehydes with alcohols was accomplished with tert-butyl hydroperoxide and 1 mol % of tris(pentafluorophenyl)borane [B(C6F5)3] to generate the corresponding esters in good to excellent yields. The present protocol represents compatibility with wide range of functional groups as well as exceptional tolerance toward acid labile protecting groups such as TBDPS, TBDMS, acetonide, and Boc.
- Guggilapu, Sravanthi Devi,Prajapti, Santosh Kumar,Babu, Bathini Nagendra
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supporting information
p. 889 - 892
(2015/02/05)
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- A general continuous flow method for palladium catalysed carbonylation reactions using single and multiple tube-in-tube gas-liquid microreactors
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A series of continuous flow chemistry processes that facilitate the palladium-catalysed carbonylation of aryl and vinyl iodides and aryl bromides with a range of alkoxy, hydroxy and amino nucleophiles is reported. Harnessing a semipermeable Teflon AF-2400 Tube-in-Tube assembly, these reactors permit the controlled transport of carbon monoxide into solution at elevated pressure to generate homogeneous flow streams, avoiding some potential issues associated with segmented flow gas-liquid reactors. As the volume of pressurised gas contained within the device is low, the hazards associated with this are potentially mitigated relative to comparable batch processes. We also show how the incorporation of a second in-line gas-flow reactor allows for the sequential introduction of two gases (carbon monoxide and a gaseous nucleophile) into the reaction stream. A Teflon AF-2400 Tube-in-Tube reactor facilitates the use of carbon monoxide in continuous-flow C-C bond forming reactions providing esters, amides, carboxylic acids, lactones and lactams. Two reactors can be used in series to permit the sequential addition of two reactive gases (CO and Me2NH) into the flow stream.
- Gross, Ulrike,Koos, Peter,O'brien, Matthew,Polyzos, Anastasios,Ley, Steven V.
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supporting information
p. 6418 - 6430
(2016/02/18)
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- Microwave-assisted synthesis of 3-substituted indoles via intramolecular arene-alkene coupling of o-iodoanilino enamines
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A generally applicable and high-yielding protocol for the synthesis of 3-substituted indole derivatives is described. Key features include microwave-assisted intramolecular arene-alkene coupling of o-iodoanilino enamines, and expedient synthesis of o-iodo
- Lee, Won-Il,Jung, Jong-Wha,Sim, Jaehoon,An, Hongchan,Suh, Young-Ger
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p. 7211 - 7219
(2013/08/23)
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- Teflon AF-2400 mediated gas-liquid contact in continuous flow methoxycarbonylations and in-line FTIR measurement of CO concentration
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We report on the development of a continuous flow process for the palladium catalysed methoxycarbonylation of aryl, heteroaromatic and vinyl iodides and an aryl bromide using a Teflon AF-2400 based Tube-in-Tube reactor to mediate the selective permeation of carbon monoxide into solution at elevated pressures. The low volume of pressurised gas within the reactor (5.6 mL) offers the potential for an enhanced safety profile compared to batch processes. We also present preliminary results for the use of in situ FTIR to measure solution concentrations of carbon monoxide and demonstrate the use of a second reactor to effect the removal of carbon monoxide from the flow stream.
- Koos, Peter,Gross, Ulrike,Polyzos, Anastasios,O'Brien, Matthew,Baxendale, Ian,Ley, Steven V.
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supporting information; experimental part
p. 6903 - 6908
(2011/10/31)
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- Indoline-3-carboxylic acid derived organocatalysts for the anti-mannich reaction
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Mannich type reactions of a preformed aldimine with various carbonyl compounds were investigated with a series of functionalised indoline derivatives as catalysts: indoline-3-carboxylic acid, the diphenylcarbinol analogue and O-protected silyl ether analo
- Pietruszka, Joerg,Simon, Robert Christian
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supporting information; experimental part
p. 14534 - 14544
(2011/03/20)
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- Substituted indole derivatives
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Substituted indole derivatives, processes for the preparation thereof, medicinal products and pharmaceutical compositions containing these compounds and the use of substituted indole derivatives to treat pain and other conditions and for other medical purposes.
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Page/Page column 13
(2009/09/07)
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- SUBSTITUTED INDOLE DERIVATIVES
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The present invention relates to substituted indole derivatives having the general formula (I) which act on the ORL 1 receptor wherein A and B mutually independently denote CH2, C=O or SO2, X stands for indolyl, unsubstituted or mono- or polysubstituted; T stands for (CR5a-cR6a-c)n, n = 1, 2 or 3, and Q stands for (CR7a-cR8a-c)m, m = 0,1, 2 or 3, processes for the preparation thereof, medicinal products containing these compounds and the use of substituted indole derivatives for the preparation of medicinal products.
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Page/Page column 31
(2009/10/18)
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- Efficient N-tert-butoxycarbonylation of indoles with di-tert-butyl dicarbonate catalyzed by cesium fluoride
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An environmentally friendly process for the tert-butoxycarbonylation of indoles with di-tert-butyl dicarbonate has been developed. Catalytic amount of cesium fluoride can accelerate this tert-butoxycarbonylation. Georg Thieme Verlag Stuttgart.
- Inahashi, Nobuyuki,Matsumiya, Ayako,Sato, Tsuneo
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p. 294 - 296
(2008/12/21)
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- Photochemistry of 2-indolyl aryl ethers: An unexpected rearrangement leading to C-C bond formation
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Two types of 2-(p-tolyloxy)indole were prepared and their reactivity was studied under photochemical conditions. The expected electrocyclization was not observed. Instead, unprecedented rearrangement products were obtained. The reaction outcome was found to depend on the viscosity of the media.
- Feldman, Ken S.,Vidulova, Daniela Boneva
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p. 1615 - 1623
(2007/10/03)
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- Unexpected products from the Fp2-catalyzed reductive cyclization of nitroaromatics bearing pendant unsaturation
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A representative o-nitroenone (Z=O) was cyclized by reduction with CO and [CpFe(CO)2]2 (Fp2) as the catalyst to give the corresponding 4-quinolone. In contrast, Baylis-Hillman adducts derived from o-nitrobenzaldehydes were
- O'Dell, David K.,Nicholas, Kenneth M.
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p. 747 - 754
(2007/10/03)
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