100377-32-0

Upstream product

• 55-22-1 pyridine-4-carboxylic acid 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 530-62-1 1,1'-carbonyldiimidazole 
• 90322-87-5 1-isonicotinoyl-1H-imidazole 
• 2459-09-8 4-pyridinecarboxylic acid, methyl ester 
• 1117-97-1 N,0-dimethylhydroxylamine 

Downstream Products

• 243640-28-0 4-(2,3-dimethoxybenzoyl)pyridine 
• 1017-24-9 2-phenyl-1-pyridin-4-yl-ethanone 
• 1283117-85-0 4-(3-ethoxy-4-hydroxy-5-nitrophenyl)-5-phenyl-6-(pyridin-4-yl)-3,4-dihydropyrimidin-2(1H)-one 
• 1552301-62-8 N-(5-(2-amino-4-(pyridin-4-yl)pyrido[2,3-d]pyrimidin-6-yl)-2-methoxypyridin-3-yl)-2,4-difluorobenzenesulfonamide 
• 1202375-44-7 2,2-dimethyl-4-(4-((5-methylpyridin-2-yl)methoxy)phenyl)-5-(pyridin-4-yl)furan-3(2H)-one 
• 1202375-45-8 4-(4-((3,5-dimethylpyridin-2-yl)methoxy)phenyl)-2,2-dimethyl-5-(pyridin-4-yl)furan-3(2H)-one 
• 1202368-23-7 2,2-dimethyl-5-(pyridin-4-yl)-4-(4-(quinolin-2-ylmethoxy)phenyl)furan-3(2H)-one 
• 1202375-46-9 4-(4-((6-fluoroquinolin-2-yl)methoxy)phenyl)-2,2-dimethyl-5-(pyridin-4-yl)furan-3(2H)-one 
• 1701-69-5 1-(4-pyridyl)-1-propanone 
• 14548-46-0 4-Benzoylpyridine 
• 1600563-64-1 C₂₆H₂₂ClN₅O 

Relevant academic research and scientific papers

Synthesis of the isonicotinoylnicotinamide scaffolds of the naturally occurring isoniazid-NAD(P) adducts

The first syntheses of the 1-hydroxy-1-(pyridin-4-yl)-1,2-dihydro-3H- pyrrolo[3,4-c]pyridin-3-one heterocycle and the 3-aminocarbonyl-4-isonicotinoyl- 1,4-dihydropyridine framework present in the isoniazid-NAD(P) adducts are described.

Studies on reactive pyridylketones formed by Weinreb transformations

A method has been developed to allow the preparation of reactive pure vinylpyridylketones and activated vinylketones, in general, to be used in further reactions, such as cycloadditions. The process is based on the Weinreb's amide transformation and includes a quarternary ammonium intermediate and subsequent elimination. Additionally, based on our previous results on the malonate alkylation of 3-nitropyridines and subsequent synthetic applications, we present the studies on the transformation of pyridyl malonate derivative 3 via the Weinreb's amide 4 and reactive methylpyridyl- (17) and allylpyridyl-ketone (6) into bis-heterocyclic products 18 and 19, and 8, 20, and 21, respectively.

NH vs. CH hydrogen bond formation in metal-organic anion receptors containing pyrrolylpyridine ligands

Anion complexation studies on a series of platinum(II) tetrakis(pyrrolylpyridine) salts demonstrate the importance of CH-anion hydrogen bonds in coordinating anionic guests in solution and the solid-state. The Royal Society of Chemistry 2005.

Photoenzymatic Hydrogenation of Heteroaromatic Olefins Using ‘Ene’-Reductases with Photoredox Catalysts

Flavin-dependent ‘ene’-reductases (EREDs) are highly selective catalysts for the asymmetric reduction of activated alkenes. This function is, however, limited to enones, enoates, and nitroalkenes using the native hydride transfer mechanism. Here we demonstrate that EREDs can reduce vinyl pyridines when irradiated with visible light in the presence of a photoredox catalyst. Experimental evidence suggests the reaction proceeds via a radical mechanism where the vinyl pyridine is reduced to the corresponding neutral benzylic radical in solution. DFT calculations reveal this radical to be “dynamically stable”, suggesting it is sufficiently long-lived to diffuse into the enzyme active site for stereoselective hydrogen atom transfer. This reduction mechanism is distinct from the native one, highlighting the opportunity to expand the synthetic capabilities of existing enzyme platforms by exploiting new mechanistic models.

Saturated Bioisosteres of ortho-Substituted Benzenes

Saturated bioisosteres of ortho-disubstituted benzenes (bicyclo[2.1.1]hexanes) were synthesized, characterized and validated. These cores were incorporated into the bioactive compounds Valsartan, Boskalid and Fluxapyroxad instead of the benzene ring. The

Casein kinase 1 (CK1) inhibitor for plants (by machine translation)

[Problem] to provide various lead compounds PHA derivatives, and/or circadian rhythm control agent having stronger CK1 inhibitor activity. [Solution] a compound represented by formula I, or a salt thereof or a solvate thereof. (R1 The, H or C1 - 5 A straight-chain, branched or cyclic alkyl group, alkenyl group or alkynyl group, R2 The, H, halogen (F, Cl, Br or I), or a C1 - 4 The alkyl group, the ring A, 5 - 8 membered lactam ring showing; however, R1 And R2 Except H together. )[Drawing] no (by machine translation)

Design, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure

Based on the co-crystal structures of tubulin with plinabulin and Compound 1 (a derivative of plinabulin), a total of 18 novel plinabulin derivatives were designed and synthesized. Their biological activities were evaluated against human pancreatic cancer BxPC-3 cell lines. Two novel Compounds 13d and 13e exhibited potent activities with IC50 at 1.56 and 1.72 nM, respectively. The tubulin polymerization assay indicated that these derivatives could inhibit microtubule polymerization. Furthermore, the interaction between tubulin and these compounds were elucidated by molecular docking. The binding modes of Compounds 13d and 13e were similar to the co-crystal structure of Compound 1. H-π interaction was observed between the aromatic hydrogen of thiophene moiety with Phe20, which could enhance their binding affinities.

Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt

A high-throughput screen of the ligand binding domain of the nuclear receptor retinoic acid-related orphan receptor gamma t (RORγt) employing a thermal shift assay yielded a quinoline tertiary alcohol hit. Optimization of the 2-, 3- and 4-positions of the quinoline core using structure-activity relationships and structure-based drug design methods led to the discovery of a series of modulators with improved RORγt inhibitory potency and inverse agonism properties.

Discovery of a novel series of thienopyrimidine as highly potent and selective PI3K inhibitors

Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway provides a promising new approach for cancer therapy. Through a rational design, a novel series of thienopyrimidine was discovered as highly pote

PHENYL LINKED QUINOLINYL MODULATORS OF RORyt

The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also