113248-64-9Relevant academic research and scientific papers
4-(N,N-diarylmethylamine)furan-2(5H)-one derivatives, and preparation method and application thereof
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Paragraph 0071, (2018/10/19)
The invention discloses 4-(N,N-diarylmethylamine)furan-2(5H)-one derivatives, and a preparation method and application thereof. The derivatives are as shown in a general formula (I) which is describedin the specification. In the formula (I), R1 is 6-chloropyridin-3-yl, pyridin-3-yl, 6-fluoropyridin-3-yl, 6-bromopyridin-3-yl or 6-trifluoromethylpyridin-3-yl; R2 is 4-chloro-3-fluorobenzyl, thienyl,2,4,5-trifluorobenzyl, 4-trifluoromethylbenzyl, 2,6-difluorobenzyl, 4-bromobenzyl, 2-chloro-6-fluorobenzyl, 2-fluorobenzyl, 3,4-difluorobenzyl, 3-chloro-4-fluorobenzyl, 3,4,5-trifluorobenzyl, 2,4,6-trifluoro Benzyl, 4-fluoro-2-methylbenzyl, 3-bromo-4-fluorobenzyl, 2-fluorobenzonitrile, 4-fluoro-3-methylbenzyl, 3,4-dichlorobenzyl, 2-chlorobenzyl, 2,4,5-trifluorobenzyl, 4-fluorobenzyl, 3-bromobenzyl, 3-chlorobenzyl, 2,3,4,5,6-pentafluorobenzyl, 4-fluoro-3-nitrobenzyl, 5-chloro-2-fluorobenzyl, cyanobenzyl, 3-nitrobenzyl or 4-((3,3-dichloroallyl)oxy)benzyl. The derivatives provided by the invention have good activity on aphids attacking broad beans; preparation process is simple; and production cost is low.
Optimized chemical probes for REV-ERBα
Trump, Ryan P.,Bresciani, Stefano,Cooper, Anthony W. J.,Tellam, James P.,Wojno, Justyna,Blaikley, John,Orband-Miller, Lisa A.,Kashatus, Jennifer A.,Boudjelal, Mohamed,Dawson, Helen C.,Loudon, Andrew,Ray, David,Grant, Daniel,Farrow, Stuart N.,Willson, Timothy M.,Tomkinson, Nicholas C. O.
, p. 4729 - 4737 (2013/07/19)
REV-ERBα has emerged as an important target for regulation of circadian rhythm and its associated physiology. Herein, we report on the optimization of a series of REV-ERBα agonists based on GSK4112 (1) for potency, selectivity, and bioavailability.(1) Potent REV-ERBα agonists 4, 10, 16, and 23 are detailed for their ability to suppress BMAL and IL-6 expression from human cells while also demonstrating excellent selectivity over LXRα. Amine 4 demonstrated in vivo bioavailability after either iv or oral dosing.
Flow synthesis of organic azides and the multistep synthesis of imines and amines using a new monolithic triphenylphosphine reagent
Smith, Catherine J.,Smith, Christopher D.,Nikbin, Nikzad,Ley, Steven V.,Baxendale, Ian R.
supporting information; experimental part, p. 1927 - 1937 (2011/04/21)
Here we describe general flow processes for the synthesis of alkyl and aryl azides, and the development of a new monolithic triphenylphosphine reagent, which provides a convenient format for the use of this versatile reagent in flow. The utility of these new tools was demonstrated by their application to a flow Staudinger aza-Wittig reaction sequence. Finally, a multistep aza-Wittig, reduction and purification flow process was designed, allowing access to amine products in an automated fashion.
