Preparation method and purpose of pyrrolone BRD4 protein inhibitor
The invention relates to the field of medicinal chemistry, in particular to pyrrolone derivatives, a preparation method of the pyrrolone derivatives, a pharmaceutical composition containing the compounds and medical purposes of the pharmaceutical composition, particularly an antitumor purpose of the pharmaceutical composition as a BRD4 protein inhibitor.
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Paragraph 0238; 0239; 0240
(2018/04/03)
The synthesis, characterization and optical properties of novel 2-Acyl 6-Arylindolizines
A series of novel 2-Acyl-6-Aryl substituted indolizine derivatives was synthesized by a novel tandem reaction between 4-Acyl-pyrrole-2-carbaldehyde derivatives and ethyl 4-bromo-3-Arylbut-2-enoate under mild conditions. The compounds were characterized using IR, 1H NMR 13C NMR and HRMS. The crystal structure of 7a was determined using single crystal X-ray crystallography. The absorption results showed that compounds 7a-e presented their absorption maxima at ca. 270 nm, while compounds 7f and 7g with a larger conjugation system exhibited red-shifted absorption character (ca. 280 nm). Fluorescence spectra revealed that these compounds exhibited blue fluorescence (434-456 nm) in dilute solutions and showed quantum yields of fluorescence between 0.02 and 0.39 in dichloromethane.
Pyrrole chemistry. XXII. A "one-pot" synthesis of some 4-acylpyrrole-2-carboxaldehydes from pyrrole
The Vilsmeier-Haack intermediates formed from pyrrole and from 1-methylpyrrole may be acylated under normal Friedel-Crafts conditions.Hydrolytic work-up then gives 4-acylpyrrole-2-carboxaldehydes in good yield.The methoxide/methanol treatment of the 4-trichloroacetylated intermediate leads to methyl 2-formylpyrrole-4-carboxylate.These are all "one-pot" syntheses from pyrrole.The formyl group has been removed from several of the products thus affording some 3-acylpyrroles in two operations.
Anderson, Hugh J.,Loader, Charles E.,Foster, Aidan
p. 2527 - 2530
(2007/10/02)
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