35856-92-9

Upstream product

• 96-43-5 2-thienyl chloride 
• 308103-40-4 (2-acetylphenyl)boronic acid 
• 554-14-3 2-Methylthiophene 
• 611-73-4 Benzoylformic acid 
• 20893-30-5 2-cyanomethylthiophene 
• 3437-95-4 2-Iodothiophene 
• 98-86-2 acetophenone 
• 93-58-3 benzoic acid methyl ester 
• 527-72-0 2-thiophenylcarboxylic acid 
• 39098-97-0 2-thienylacetic acid chloride 
• 71-43-2 benzene 
• 1918-77-0 Thiophene-2-acetic acid 

Downstream Products

• 1569839-59-3 methyl 2-oxo-6-phenyl-5-(2-thienyl)-2H-pyran-3-carboxylate 
• 98-03-3 thiophene-2-carbaldehyde 
• 93-98-1 N-phenyl benzoyl amide 
• 58255-22-4 rac-1-phenyl-2-(thiophen-2-yl)ethanol 
• 30135-07-0 1-phenyl-2-(2-thienyl)ethanedione 
• 2005-08-5 4-chlorophenyl benzoate 
• 1593235-59-6 6,7-dimethoxy-4-(2-thienylmethyl)quinazoline 
• 91344-57-9 1-[5-(2-thienylmethyl)-2-furanyl]ethanone 
• 93-99-2 benzoic acid phenyl ester 
• 99969-93-4 2-(thiophen-2-ylmethyl)benzoxazole 
• 1283117-01-0 4-(3-ethoxy-4-hydroxy-5-nitrophenyl)-6-phenyl-5-(thiophen-2-yl)-3,4-dihydropyrimidin-2(1H)-one 

Relevant academic research and scientific papers

Asymmetric transfer hydrogenation of heterocycle-containing acetophenone derivatives using N-functionalised [(benzene)Ru(II)(TsDPEN)] complexes

The application of enantiomerically-pure ruthenium(II) catalysts containing N - functionalised TsDPEN ligand to the asymmetric transfer hydrogenation of 15 examples of α-heterocyclic acetophenone derivatives is reported. Products of up to 99% ee were formed.

N-heterocyclic carbene-palladium-imine complex catalyzed α-arylation of ketones with aryl and heteroaryl chlorides under air atmosphere

A new structure of saturated ring skeleton monoligated NHC-Pd-Imine complex was easily synthesized and unambiguously confirmed by X-ray single crystal diffraction. It was found to be an efficient and air-stable catalyst for the α-arylation of ketones. The reaction could be operated in air without any negative effect. Non-activated aryl and heteroaryl chlorides have been successfully applied in the reaction with only 0.5 mol% catalyst loadings under air atmosphere. Excellent to good product yields were afforded.

Palladium-Catalyzed Direct α-C(sp3) Heteroarylation of Ketones under Microwave Irradiation

Heteroaryl compounds are valuable building blocks in medicinal chemistry and chemical industry. A palladium-catalyzed direct α-C(sp3) heteroarylation of ketones under microwave irradiation is developed and reported in this study. Under optimized condition

Two-Step One-Pot Synthesis of Unsymmetrical (Hetero)Aryl 1,2-Diketones by Addition-Oxygenation of Potassium Aryltrifluoroborates to (Hetero)Arylacetonitriles

An efficient one-pot two-step procedure for the synthesis of unsymmetrical (hetero)aryl 1,2-diketones has been developed. The reaction proceeds through a palladium-catalyzed nucleophilic addition of potassium aryltrifluoroborates to aliphatic nitriles followed by a copper-catalyzed aerobic benzylic C–H oxygenation using molecular oxygen as a green oxidant. This represents the first example of the direct synthesis of unsymmetrical diaryl 1,2-diketones from arylacetonitriles. This method utilizes inexpensive, stable, nontoxic, and readily available starting materials, is highly effective in the presence of both electron-rich and electron-poor nitriles and aryltrifluoroborates, and tolerates a wide variety of functional groups. The synthetic utility of this transformation was shown by increasing the scale of the reaction and by carrying out the one-pot protocol for the preparation of quinoxaline and benzimidazole derivatives. A plausible reaction mechanism has also been proposed.

Metal-free, one-pot synthesis of allylic and benzylic esters via decarboxylation and C-H bond activation

A tetrabutylammonium iodide catalyzed method has been developed for the one-pot synthesis of allylic and benzylic esters from α-oxo carboxylic acids and alkenes/alkylbenzenes via decarboxylation and C-H bond activation. Various allylic and benzylic esters were obtained in good yield.

Synthesis of 6-substituted 3-(alkoxycarbonyl)-5-aryl-α-pyrones

An efficient synthesis of 6-substituted 3-(alkoxycarbonyl)-5-aryl-α- pyrones is reported. This methodology consists of the successive manipulation of an addition-elimination reaction between benzyl ketone derivatives and dimethyl methoxymethylenemalonate,

Room-temperature Suzuki-Miyaura coupling of heteroaryl chlorides and tosylates

Suzuki-Miyaura coupling of heteroaryls is an important method for the preparation of compound libraries for medicinal chemistry and materials research. Although many catalysts have been developed, none of them have been generally applicable to the coupling reactions of heteroaryl chlorides and tosylates at room temperature. We discovered that a catalyst combination of Pd(OAc)2 and XPhos (2-dicyclohexylphosphanyl-2',4',6'- triisopropylbiphenyl) could efficiently catalyze these couplings. Besides the choice of catalyst, the use of hydroxide bases in an aqueous alcoholic solvent was essential for fast couplings. These conditions promoted fast release of active catalyst (XPhos)Pd0, and accelerated the transmetalation in the catalytic cycle. Most of the major families of heteroaryl chlorides (31 examples) and tosylates (17 examples) reached full conversion within minutes to hours at room temperature. The method could be easily scaled up for gram-scale synthesis. Furthermore, we examined the relative reactivity of coupling partners in whole reactions. Electron-rich heteroaryl chlorides and tosylates reacted more slowly than electron-deficient ones, in the order of indole, pyrrole furan, thiophene > pyridine. Similarly, electron-deficient arylboronic acids were less reactive than electron-neutral and electron-rich ones. The reactivity trends from this study can help to choose appropriate coupling partners for Suzuki reactions.

NOVEL DIHYDROPYRIMIDIN-2(1H)-ONE COMPOUNDS AS S-NITROSOGLUTATHIONE REDUCTASE INHIBITORS

The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: p