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• 7377-26-6 4-Methoxycarbonylbenzoyl chloride 
• 1257841-78-3 2-(4-methoxycarbonylbenzoyloxy)-1-methylpyridinium triflate 
• 42967-55-5 monomethyl monopotassium terephthalate 
• 120-61-6 1,4-benzenedicarboxylic acid dimethyl ester 

Relevant academic research and scientific papers

Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities

In this study, we report the design and synthesis of a series of novel thiophene-arylamide compounds derived from the noncovalent decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1) inhibitor TCA1 through a structure-based scaffold hopping strategy. Systematic optimization of the two side chains flanking the thiophene core led to new lead compounds bearing a thiophene-arylamide scaffold with potent antimycobacterial activity and low cytotoxicity. Compounds 23j, 24f, 25a, and 25b exhibited potent in vitro activity against both drug-susceptible (minimum inhibitory concentration (MIC) = 0.02-0.12 μg/mL) and drug-resistant (MIC = 0.031-0.24 μg/mL) tuberculosis strains while retaining potent DprE1 inhibition (half maximal inhibitory concentration (IC50) = 0.2-0.9 μg/mL) and good intracellular antimycobacterial activity. In addition, these compounds showed good hepatocyte stability and low inhibition of the human ether-à-go-go related gene (hERG) channel. The representative compound 25a with acceptable pharmacokinetic property demonstrated significant bactericidal activity in an acute mouse model of tuberculosis. Moreover, the molecular docking study of template compound 23j provides new insight into the discovery of novel antitubercular agents targeting DprE1.

THERMOPLASTIC POLYMER COMPOSITION

The invention provides a thermoplastic polymer composition comprising a polyolefin polymer and a nucleating agent. The nucleating agent comprises a compound conforming to the structure of Formula (I). The invention also provides a series of compounds encompassed by the structure of Formula (I).

THERMOPLASTIC POLYMER COMPOSITION

The invention provides a compound conforming to the structure of Formula (CX). The invention also provides a thermoplastic polymer composition comprising a polyolefin polymer and a compound conforming to the structure of Formula (CX) as a nucleating agent.

Thermoplastic polymer composition

The invention provides a compound conforming to the structure of Formula (C) The invention also provides a thermoplastic polymer composition comprising a polyolefin polymer and a compound conforming to the structure of Formula (C) as a nucleating agent.

Controlled and chemoselective reduction of secondary amides

This communication describes a metal-free methodology involving an efficient and controlled reduction of secondary amides to imines, aldehydes, and amines in good to excellent yields under ambient pressure and temperature. The process includes a chemoselective activation of a secondary amide with triflic anhydride in the presence of 2-fluoropyridine. The electrophilic activated amide can then be reduced to the corresponding iminium using triethylsilane, a cheap, rather inert, and commercially available reagent. Imines can be isolated after a basic workup or readily transformed to the aldehydes following an acidic workup. The amine moiety can be accessed via a sequential reductive amination by the addition of silane and Hantzsch ester hydride in a one-pot reaction. Moreover, this reduction tolerates various functional groups that are usually reactive under reductive conditions and is very selective to secondary amides.

Selective deprotection and amidation of 2-pyridyl esters via N-methylation

The 2-pyridyl residue serves as a protecting group for various carboxylic acids. The protecting group is selectively cleaved under mild conditions via N-methylation of the pyridyl group. During the deprotection process, the various functional groups as we

Acid-catalysed N-alkyl heterolysis of tertiary pyridinecarboxamides and benzamides under mild conditions

Tertiary pyridinecarboxamides 1-9 and related benzamides 10-18 bearing a tert-butyl substituent were found to undergo alkyl-nitrogen heterolysis under unusually mild conditions. Accordingly, the corresponding secondary amides 19-33 have been isolated in high yields as the sole reaction product. Through a kinetic study based on pH-rate profiles and activation parameters, we have shown that the alkyl-nitrogen fission involved an initial protonation of the amide group that would concern the oxygen atom.