74295-19-5

Upstream product

• 150-75-4 N-methyl-p-aminophenol 
• 108-24-7 acetic anhydride 
• 75-36-5 acetyl chloride 
• 2436-77-3 4-(N,N-dimethylamino)phenyl acetate 
• 579-10-2 N-acetyl-N-methylaniline 
• 64-19-7 acetic acid 
• 579-58-8 N-methyl-(4-acetamido)phenol 

Downstream Products

• 579-58-8 N-methyl-(4-acetamido)phenol 

Relevant academic research and scientific papers

Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics

We report the optimisation of a series of novel amide-piperidine (piperazine) derivatives using the multiple ligand approach with dopamine and serotonin receptors. Of the derivatives, compound 11 exhibited high affinity for the D2, 5-HT1A, and 5-HT2A receptors, but low affinity for the 5-HT2C and histamine H1 receptors and human ether-a-go-go-related gene (hERG) channels. In vivo, compound 11 reduced apomorphine-induced climbing, MK-801-induced hyperactivity and DOI-induced head twitching without observable catalepsy, even at the highest dose tested. In addition, it exhibited suppression in a CAR test. Furthermore, in a novel object recognition task, it displayed procognition properties. Therefore, compound 11 is a promising candidate multi-target antipsychotic.

Thermolysis and radiofluorination of diaryliodonium salts derived from anilines

Aniline-derived diaryliodonium salts were synthesized and functionalized in good to excellent yields by judicious utilization of electron-withdrawing protecting groups. This simple approach opens another route to radiolabeling amino arenes in relatively complex molecules, such as flutemetamol.

The copper-catalyzed aerobic oxidative amidation of tertiary amines

A general and efficient method for the synthesis of tertiary amides has been developed via the copper-catalyzed aerobic oxidative amidation of tertiary amines. Due to the use of the O2 oxidant, various functional groups were well tolerated under the present conditions. Extensive substrates studies demonstrated its potential as a practical approach for the synthesis of tertiary amides.

Direct acetoxylation and etherification of anilides using phenyliodine bis(trifluoroacetate)

Treatment of various anilides with 1.5 equiv. of phenyliodine bis(trifluoroacetate) (PIFA) and 1.0 equiv. of BF3·OEt 2 in AcOH at room temperature afforded the corresponding para-acetoxylated products with high regioselectivity. In addition, this reaction could be expanded to the etherification of anilides. In the presence of 2.0 equiv. of PIFA and 2.0 equiv. of BF3·OEt2, the reaction of anilides with alcohols provided the corresponding para-etherified products in good yields. The Royal Society of Chemistry 2011.

Retention behavior of compounds with active hydrogen atoms and their acetylated derivatives in reversed-phase HPLC

In view of poor interlaboratory reproducibility of retention indices I in reversed-phase high-performance liquid chromatography, not the indices themselves but their differences for reactants and products of interaction with various reagents can be used to identify compounds with active hydrogen atoms. For acetylated derivatives of phenols and aromatic amines, the quantity ?I = I(ArXH) -I(ArXCOCH3), where X = O or NH. has statistically significant distinguishable values of 126 ± 15 and 70 ± 20, respectively. The additivity of the parameters ?I is first revealed for the polyfunctional compounds of these classes that are incapable of intramolecular hydrogen bonding. Abnormal ?I values and deviations from the additivity rule are observed only for substances with intramolecular hydrogen bonding. This finding can be used to confirm the presence of relevant structural units in molecules.

Fungicidal 2-aryl-2-cyano-2-(aryloxyalkyl)ethyl-1,2-4-triazoles

2-aryl-2-cyano-2-(aryloxyalkyl)ethyl-1,2,4-triazoles of the formula STR1 wherein Ar1 and Ar2 are optionally substituted aryl groups which may or may not be different, R is hydrogen or alkyl, n is an integer of at least one, and the agronomically acceptable enantiomorphs, acid addition salts and metal salt complexes thereof, compositions containing these compounds and their uses as fungicides, particularly against phytopathogenic fungi.