19482-08-7

Upstream product

• 95-74-9 3-chloro-p-toluidine 
• 71-43-2 benzene 
• 83846-48-4 3-chloro-4-methyliodobenzene 
• 98-80-6 phenylboronic acid 
• 497-19-8 sodium carbonate 
• 95-73-8 2,4-dichlorotoluene 
• 100-59-4 phenylmagnesium chloride 
• 591-50-4 iodobenzene 
• 175883-63-3 B-(3-chloro-4-methylphenyl)boronic acid 
• 933674-79-4 C₁₃H₈ClF₃ 
• 89794-02-5 4-bromo-2-chlorotoluene 

Downstream Products

• 219767-59-6 3-(2-chloro-4-phenylbenzyl)-2,7-dimethyl-3H-imidazo[4,5-b]pyridine-5-carboxylic acid 
• 219764-07-5 6-carboxy-1-(2-chloro-4-phenylbenzyl)-3-methyl-1H-indazole 

Relevant academic research and scientific papers

Anchored Pd(0) Nanoparticles on Synthetic Talc for the Synthesis of Biaryls and a Precursor of Angiotensin II Inhibitors

The palladium-catalyzed Suzuki-Miyaura cross-coupling reaction is one of the most important and efficient reactions to prepare a variety of organic compounds, including biaryls. Despite the overwhelming number of reports related to this topic, some methodological difficulties persist in terms of catalyst handling, recovery, and reuse, as well as the reaction media. This work reports the rational design of new, efficient, cost-effective, and reusable palladium catalysts supported on synthetic talc for the Suzuki-Miyaura reaction. From the results, key points were identified: both designed catalysts accelerated the reaction in EtOH and an open-flask setup, affording moderate to excellent yields within a short time (e.g., 30 min) even for deactivated aryl halides; the protocol can be applied to a great number of both cross-coupling partners, showing an excellent functional group tolerance; the catalysts can be recovered and reused without significant loss of activity. This protocol was used for the synthesis of a precursor of angiotensin II inhibitors such as valsartan, losartan, irbesartan, and telmisartan.

EFFICIENT CATALYST FOR THE FORMATION OF POLYARYL HYDROCARBONS SUITABLE AS PRECURSORS FOR POLYDENTATE ORGANOPHOSPHORUS CATALYST LIGANDS

The disclosure relates to the efficient preparation of aromatic hydrocarbons useful as intermediates for di-, tri-, tetra- and poly-dentate organophosphorus ligands having value in particular as hydroformylation catalysts. The use of triarylphosphine halide catalysts have been found to be more efficient in forming these intermediates by the use of excess triarylphosphine in an amount beyond what is required to form a coordination complex.

Ligand Dependent Switch from RXR Homo- to RXR-NURR1 Heterodimerization

Retinoid X receptors (RXRs) play key roles in many physiological processes in both the periphery and central nervous system. In addition, RXRs form heterodimers with other nuclear receptors to exert their physiological effects. The nuclear receptor relate

Hydrodefluorinations of trifluorotoluenes by LiAlH4 and TiCl4

In the presence of 2 mol% of TiCl4, α,α,α- trifluorotoluene derivatives were reduced with LiAlH4 to furnish toluene derivatives in high yields. Selective reduction of bis(trifluoromethyl) benzene derivative is effected. The difference of the reactivity between TiCl4 and NbCl5 is also discussed.

Dialkylimidazole inhibitors of Trypanosoma cruzi sterol 14α-demethylase as anti-Chagas disease agents

New dialkylimidazole based sterol 14α-demethylase inhibitors were prepared and tested as potential anti-Trypanosoma cruzi agents. Previous studies had identified compound 2 as the most potent and selective inhibitor against parasite cultures. In addition, animal studies had demonstrated that compound 2 is highly efficacious in the acute model of the disease. However, compound 2 has a high molecular weight and high hydrophobicity, issues addressed here. Systematic modifications were carried out at four positions on the scaffold and several inhibitors were identified which are highly potent (EC50 1 nM) against T. cruzi in culture. The halogenated derivatives 36j, 36k, and 36p, display excellent activity against T. cruzi amastigotes, with reduced molecular weight and lipophilicity, and exhibit suitable physicochemical properties for an oral drug candidate.

Sulfonamide compounds and uses thereof as medicines

The present invention relates to a sulfonamide compound of the formula (I): wherein each symbol is as defined in the specification, a salt thereof, and a pharmaceutical composition containing same. This compound can be an effective agent for the prophylaxis and treatment of the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy suppressing action.

Sulfonamide compounds and medicinal use thereof

A sulfonamide compound of the formula (I):R 1 --SO 2 NHCO--A--R 2 (I)wherein R 1 is alkyl, alkenyl, alkynyl and the like; A is an optionally substituted heteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyl and 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R 2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.

IMIDAZOLE COMPOUNDS AND MEDICINAL USE THEREOF

Imidazole compounds represented by general formula (I): wherein each symbol is as defined in the specification, and salts thereof, and a pharmaceutical composition containing same are provided. These compounds are useful in treating the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy inhibitory action.