The functionalization of heteroarenes has been integral to the structural diversification of medicinally active molecules such as quinolines, pyridines, and phenanthridines. Electron-deficient heteroarenes are electronically compatible to react with relatively nucleophilic free radicals such as hydroxyalkyl. However, the radical functionalization of such heteroarenes has been marked by the use ...

Since the first synthesis of trifluoromethyl ethers in 1935, the trifluoromethoxy (OCF3) group has made a remarkable impact in medicinal, agrochemical, and materials science research. However, our inability to facilely incorporate the OCF3 group into molecules, especially heteroaromatics, has limited its potential across a broad spectrum of technological applications. Herein, we report a scalab...

The combination of α-acetamidocinnamic acid (HACA) and different N , pyridines (dPy) leads to crowded Zn( ii ) metal centers. increasing bulkiness competes with the chelation enhanced effect (CHEF) in resulting quantum yields.

An effective and direct synthetic strategy for a new series of functionalized mono-, bis-, spiro[1,2,4]triazolo[1,5-a]pyridines from 1,2-diaminopyridine precursor has been described. Reaction o...

Abnormal dopamine signaling in brain has been implicated in several conditions such as cocaine abuse, Parkinson's disease and depression. Potent and selective dopamine transporter inhibitors may be useful as pharmacological tools and therapeutic agents. Simple substituted pyridines were discovered as novel dopamine transporter (DAT) inhibitors through pharmacophore-based 3D-database search. The...

Rate and equilibrium constants for the reactions of pyridines with donor-substituted benzhydrylium ions have been determined spectrophotometrically. The correlation equation log k(20 degrees C)=s(N+E), in which s and N are nucleophile-specific parameters and E is an electrophile-specific parameter, has been used to determine the nucleophilicity parameters of various pyridines in CH(2)Cl(2) and ...

One-pot and facile preparations of 6-(2-hydroxy-5-R-benzoyl)-4-methyl-2-R1- pyrazolo[3,4-b]pyridines 4a-o are described, using the reaction of 3-formyl chromones 1 with 5-amino-1-R1-pyrazoles 2. An enamine-intermediate 2-ethyloxy-6-R-3-(3-methyl-1- phenylpyrazol-5-ylaminomethylene)chroman-4-one 3 was isolated at lower temperatures. Acyloxy-derivatives 5 of compounds 4 were obtained by acylation...

Strongly halogen-bonded complexes form between 4-alkoxyphenyl-4-pyridines and iodine as well the interhalogens ICl IBr. Examples are characterised by single crystal X-ray crystallography most show a liquid-crystalline SmA phase.

Transition-metal-catalyzed [2+2+2] cycloaddition reactions that use two alkynes and a nitrile is the most straightforward and powerful strategy for the construction of multisubstituted pyridines with high atom efficiency. The iron-catalyzed [2+2+2] cycloaddition to form pyridines remains a great challenge in this field, although significant efforts have been made in various catalytic systems (e...

The relative gas-phase halogen cation affinities of a group of substituted pyridines have been ordered, and absolute C1+ affinity values have been estimated. The C1+-bound dimer of two pyridines is generated in an ion/molecule reaction using mass-selected Cl-C=O+ as the chlorinating agent, and its competitive fragmentations to yield the C1+-pyridine monomers are monitored by multiple-stage (MS3...