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Upstream product

• 29681-44-5 5-bromo-3-pyridine carboxylic acid methyl ester 
• 7486-35-3 tri-n-butyl(vinyl)tin 
• 668987-20-0 methyl 1-acetyl-4-[(β-carbolin-1-yl)methyl]-5-vinyl-1,4-dihydropyridine-3-carboxylate 
• 75927-49-0 pinacol vinylboronate 
• 29681-42-3 methyl 4-bromopyridine-2-carboxylate 
• 128-37-0 2,6-di-tert-butyl-4-methyl-phenol 
• 108-05-4 vinyl acetate 

Relevant academic research and scientific papers

Nickel-Catalyzed Reductive Cross-Coupling of Aryl Bromides with Vinyl Acetate in Dimethyl Isosorbide as a Sustainable Solvent

A nickel-catalyzed reductive cross-coupling has been achieved using (hetero)aryl bromides and vinyl acetate as the coupling partners. This mild, applicable method provides a reliable access to a variety of vinyl arenes, heteroarenes, and benzoheterocycles, which should expand the chemical space of precursors to fine chemicals and polymers. Importantly, a sustainable solvent, dimethyl isosorbide, is used, making this protocol more attractive from the point of view of green chemistry.

NOVEL HISTONE METHYLTRANSFERASE INHIBITORS

The present invention relates to novel compounds of formula (I) as defined herein. The compounds are inhibitors of histone methyltransferases of the seven-beta-strand family, in particular of KMT9.

Azologization and repurposing of a hetero-stilbene-based kinase inhibitor: Towards the design of photoswitchable sirtuin inhibitors

The use of light as an external trigger to change ligand shape and as a result its bioactivity, allows the probing of pharmacologically relevant systems with spatiotemporal resolution. A hetero-stilbene lead resulting from the screening of a compound that was originally designed as kinase inhibitor served as a starting point for the design of photoswitchable sirtuin inhibitors. Because the original stilbenoid structure exerted unfavourable photochemical characteristics it was remodelled to its heteroarylic diazeno analogue. By this intramolecular azologization, the shape of the molecule was left unaltered, whereas the photoswitching ability was improved. As anticipated, the highly analogous compound showed similar activity in its thermodynamically stable stretched-out (E)-form. Irradiation of this isomer triggers isomerisation to the long-lived (Z)-configuration with a bent geometry causing a considerably shorter end‐to‐end distance. The resulting affinity shifts are intended to enable real‐time photomodulation of sirtuins in vitro.

Pd-Catalyzed Vinylation of Aryl Halides with Inexpensive Organosilicon Reagents Under Mild Conditions

Pd-catalyzed Hiyama vinylation reaction of non-activated aryl chlorides and bromides under mild conditions was developed. The use of efficient vinyl donors and electron-rich sterically hindered phosphine ligands was critical for the success of the reaction. The products of this transformation can be used for Am/Cm separation, an important challenge in nuclear fuel reprocessing. The substituent effect on Am/Cm separating selectivity was also achieved, which could contribute to the development of new chromatographic materials for the separation of Am and Cm.

HETEROCYCLIC FXR MODULATORS

The present technology is directed to compounds of formula (I), compositions, and methods related to modulation of FXR. In particular, the present compounds and compositions may be used to treat FXR-mediated disorders and conditions, including, e.g., liver disease, hyperlipidemia, hypercholesteremia, obesity, metabolic syndrome, cardiovascular disease, gastrointestinal disease, and atherosclerosis, and renal disease.

Aza-stilbenes as potent and selective c-RAF inhibitors

The synthesis of several novel aza-stilbene derivatives was carried out. The compounds were tested for their c-RAF enzyme inhibition. Compound 27 possesses significant potency against c-RAF and demonstrates selectivity over other protein kinases. A hypoth

Total Synthesis of the Proposed Structures of Indole Alkaloids Lyaline and Lyadine

The harman-1,4-dihydropyridines 1 and 2, which constitute the originally proposed structures for the indole alkaloids lyaline and lyadine, have been synthesized, and their NMR data have been compared with those available for the natural products. Due to the discrepancies in the spectral data, the structures of lyadine and lyaline should be revised.

Total Syntheses and Antimicrobial Activities of Pyridine Alkaloids from Rubiaceae

Pyridine alkaloids from Rubiaceae were prepared by palladium-catalyzed cross-coupling reactions of methyl 5-bromonicotinate (6) with various organometallic reagents.Baker's yeast reduction of the ketone 8 gave the levorotatory alcohol (S)-1.On this basis, the naturally occuring alcohol (+)-1 was assigned to be (R)-configurated.The alkaloids 1 and 4 show weak antimicrobial activities. - Keywords: Pyridine alkaloids; Palladium catalyst; Baker's yeast; Antimicrobial activity