71794-43-9

Upstream product

• 100-61-8 N-methylaniline 
• 29688-78-6 N-methylanilinium sulfate 
• 1220125-39-2 3-{methyl[(2-nitrophenyl)sulfonyl]amino}benzenesulfonic acid 
• 1220125-38-1 3-[(2-nitrophenyl)sulfonyl]aminobenzenesulfonic acid 
• 121-47-1 3-aminobenzenesulfonic acid 
• 70916-29-9 N-methylorthanilic acid 
• 24447-99-2 N-methylsulphanilic acid 
• 29688-78-6 N-methyl-N-phenylammonium sulfate 

Downstream Products

• 14703-69-6 3-(N-methylamino)phenol 

Relevant academic research and scientific papers

GLUTAMATE DERIVATIVES OR SALTS THEREOF

Compounds having an excellent CaSR agonist activity are in demand. The invention provides glutamate derivatives or salts thereof, pharmaceutical compositions comprising the glutamate derivatives, preventive or therapeutic agents for diarrhea, hyperparathyroidism or peptic ulcer.

PROPHYLACTIC AGENT OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY

A medicament having an excellent CaSR agonist action which enables the prevention or treatment of diabetes or obesity is provided by a composition comprising the compound represented by general formula (I) as defined, or a salt thereof.

CASR AGONIST

By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof.

ISOMERIC TRANSFORMATIONS OF AMINOSULFONIC ACIDS OF THE BENZENE SERIES IN MIXTURES OF SULFURIC AND ACETIC ACIDS

The isomerization rate of aminosulfonic acids in anhydrous binary mixtures of sulfuric and acetic acids is lower than in aqueous sulfuric acid solutions but higher than in 100percent sulfuric acid.This is explained by the differences in the structure and activity of the proton carriers during desulfonation.The rate of transformation of the labile isomers into the meta isomers increases with increase in the acidity of the medium, and this is due to the increase in the resulfonation rate of the protonating molecules of the amines formed during the desulfonation of the aminosulfonic acids.The effect of mercuric sulfate on the isomeric transformations of aminosulfonic acids is explained by the mercuration of the protonated molecules of the amines, which takes place at higher rates than their sulfonation and leads to the formation of the meta-mercury derivatives of the amines.The latter are than converted into the m-aminosulfonic acids by the action of concentrated sulfuric acid.

KINETIC OF THE SULFONATION OF AMINES OF THE BENZENE SERIES WITH SULFURIC ACID

The kinetics of the sulfonation of primary, secondary, and tertiary amines of the benzene series with 80-99.7percent sulfuric acid were investigated.It was shown that the unprotonated and protonated forms of the amines, which are present in equilibrium, undergo sulfonation.The effective reaction rate constants and the activation energies for the sulfonation of the unprotonated and protonated molecules of the amines were calculated.The reaction mechanism and the structure of the transition state are discussed.

MECHANISM OF THE SULFONATION OF AROMATIC AMINES BY SULFURIC ACID AT HIGH TEMPERATURES

The kinetics of the rearrangement of unsubstituted and N-substituted phenylammonium hydrogen sulfates to the corresponding aminosulfonic acids of the benzene series were studied.The isomeric composition of the reaction products formed during the sulfonation of amines of the benzene series by various amounts of 100percent H2SO4 was also studied.The rearrangement is described by a second-order kinetic equation.Its effective rate constant at various temperatures and the activation energies were calculated.It is suggested that the sulfonation of aromatic amines by an equimolar amount of sulfuric acid at high temperatures takes place through the dissociation of the arylammonium hydrogen sulfates with the formation of arylamines and sulfuric acid and subsequent direct sulfonation of the arylamines by the sulfuric acid.