- Novel Myocyte Enhancer Factor 2 (MEF2) modulators
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The present disclosure provides novel compounds capable of functioning as Myoctye Enhancer Factor 2 (MEF2) modulators, as well as compositions, pharmaceutical formulations, methods of synthesis and kits. Also provided are methods of treating a condition regulatable by MEF2 and/or MEF2 cofactors using the compounds, compositions, pharmaceutical formulations, and kits provided herein.
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Paragraph 0105-0107
(2019/08/20)
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- The synthesis of di-carboxylate esters using continuous flow vortex fluidics
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A vortex fluidic device (VFD) is effective in mediating the synthesis of di-esters at room temperature. Processing under ambient conditions allows for a simple and efficient synthesis, whilst operating under continuous flow addresses scalability. The rotational speed of the sample tube and the flow rate were critical variables during reaction optimization, and this relates to the behaviour of the fluid flow at a molecular level. Whilst at specific rotational speeds the tube imparts a vibrational response into the fluid flow, the flow rate dictates residence time and the ability to maintain high levels of shear stress. The combination of mechanically induced vibrations, rapid micromixing, high levels of shear stress and water evaporation results in yields up to 90% for 3.25 minutes or less residence time. These results are key for devising greener and more efficient processes both mediated by the VFD and other continuous flow platforms.
- Britton, Joshua,Dalziel, Stuart B.,Raston, Colin L.
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p. 2193 - 2200
(2016/04/19)
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- NOVEL TRANSCRIPTION FACTOR MODULATORS
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The present disclosure provides novel compounds capable of functioning as transcription factor modulators, as well as compositions, pharmaceutical formulations, and kits. Also provided are methods of treating a condition regulatable by a transcription factor and/or cofactor using the compounds, compositions, pharmaceutical formulations, and kits provided herein.
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Paragraph 0178; 0181; 0182
(2014/09/29)
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- Catalytic synthesis of diethyl pimelate with functionalized ionic liquids
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An acidic ionic liquid, [Emim]HSO4, was prepared and used as solvent and catalyst in the esterification reaction of 1,7-pimelic acid and ethanol. The esterification products could be easily separated from the reaction system. The effects of the reaction conditions on the reaction results, such as the amount of catalyst, molar ratio of acid and ethanol, reaction time, were examined and the optimal conditions were obtained through orthogonal tests based on single-factor experiments. The optimal conditions were as follows: n(C 2H5OH):n(C7H12O4) = 3:1, 2 mL of catalyst, reaction time for 5 h at 383.15 K. Under the optimal reaction conditions, the diethyl pimelate was obtained in 96.37 % yield. The acidic ionic liquid, [Emin]HSO4 could be reused for 5 times and the yield of diethyl pimelate were more than 95.18 % after repeating 5 times of catalyst applications. Compared with the traditional catalyst of concentrated sulfuric acid, the ionic liquids had the advantages of good chemical stability, non-pollution, less side reaction, good repeatability and not using organic solvent as hydrated solvent, etc.
- Li, Hua,Zhao, Zhengui,Zhang, Ningning,Tang, Qianqian
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experimental part
p. 2172 - 2174
(2012/03/09)
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- Highly chemoselective, oxyvanadium-catalysed cleavage of α-hydroxy ketones
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α-Hydroxy ketones (α-ketols) can be cleaved chemoselectively with a catalytic amount of dichloroethoxyoxyvanadium under an oxygen atmosphere.
- Kirihara, Masayuki,Takizawa, Shinobu,Momose, Takefumi
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- α-nitrocycloalkanones as a source of α,ω,-dicarboxylic acid dimethyl esters
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α,ω-Dicarboxylic acid dimethyl esters arc easily obtained by ring cleavage of α-nitrocycloalkanones. Thus, reaction of the latter compounds with three equivalents of potassium persulfate, in methanol and in presence of sulfuric acid at 80 °C, provides α,ω-dicarboxylic acid dimethyl esters in high yields. Long-chain, and alkylated α,ω-dicarboxylic acid dimethyl esters can be also efficiently obtained.
- Ballini, Roberto,Bosica, Giovanna
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p. 16131 - 16138
(2007/10/03)
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- A New Coupling Reaction of Alkyl Iodides with Electron Deficient Alkenes Nickel Boride (cat.) - Borohydride Exchange Resin in Methanol
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The radical addition reaction of alkyl iodides with α,β-unsaturated esters, nitriles, and ketones proceeds in moderate to excellent yields (50-95%) using Ni(OAc)2 (0.05-0.2 equiv) - BER (3-5 equiv) in methanol in 1-9 h at room temperature or at 65°C. Nickel boride on borohydride exchange resin (BER) is a good alternative reagent to tributyltin hydride for the coupling of alkyl iodides with the electron deficient alkenes in methanol. Compared with tributyltin hydride method, this method has an advantage of simple workup, since nickel boride - BER can be removed readily by filtration.
- Sim, Tae Bo,Choi, Jaesung,Joung, Meyoung Ju,Yoon, Nung Min
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p. 2357 - 2361
(2007/10/03)
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- Oxovanadium(V)-Induced Ring-Opening Oxygenation of Cyclic Ketones in Alcohol
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Cyclic ketones underwent ring-opening oxygenation on treatment with VO(OEt)Cl2 in alcohol under oxygen to give the corresponding keto ester or diesters depending on the substituent at 2-position.This system was applicable to a catalytic reaction.
- Hirao, Toshikazu,Mori, Makoto,Ohshiro, Yoshiki
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p. 2399 - 2400
(2007/10/02)
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