The 2-, 3-, and 4-methoxyamphetamines and methoxymethamphetamines were prepared and analyzed by GC-MS. Regioisomerism at the aromatic ring in these compounds possess similar analytical properties. They show similar gas chromatographic retention properties on a column with phenylmethylsilicone (HP-5) stationary phase. The mass spectra for the underivatized amines are similar and fail to provide ...

The synthesis of 1,4-diamines containing the (Z)-1,4-diaminobut-2-ene subunit via a temporary phosphorus tether/RCM strategy is described. We have developed a new method utilizing phosphorus nuclei as suitable temporary tethers for the coupling of nonracemic allylic amines. This approach allows for the generation of C(2)-symmetric and unsymmetric 1,4-diamines 1-3, which may have considerable sy...

Amines are the most important building blocks employed in modern medicinal chemistry. Secondary amines are regularly prepared by the alkylation or reductive amination of the parent amines through transition metal, typically precious metals, catalyzed reactions. In the past few years, the catalytic alkylation of amines with alcohols under hydrogenborrowing conditions as well as the catalytic red...

The synthesis of a series of benzimidazole-N-benzylpropan-1-amines and adenine-N-benzylpropan-1-amines is described. Subsequent evaluation against two strains of the anaerobic bacterium Clostridium difficile was performed with three amine derivatives displaying MIC values of 16 μg/mL. Molecular docking studies of the described amines determined that the amines interact within two active site po...

Many lipophilic amine compounds are rapidly extracted from the blood on passage through the pulmonary circulation. The extent of their extraction in normal lungs depends on their physical-chemical properties, which affect their degree of ionization, lipophilicity, and propensity for interacting with blood and tissue constituents. The hypothesis of the present study was that changes in the tissu...

Azo dyes in textiles may release aromatic amines after enzymatic cleavage by skin bacteria or after dermal absorption and metabolism in the human body. From the 896 azo dyes with known chemical structure in the available textile dyes database, 426 azo dyes (48%) can generate one or more of the 22 regulated aromatic amines in the European Union in Annex XVII of REACH. Another 470 azo dyes (52%) ...

N-Substituted 2-acetylamino-2-ethoxycarbonyl-3-(2-furyl)propanamides (8) were synthesized through the reaction of amines (13) with 2-acetylamino-2-ethoxycarbonyl-3-(2-furyl)propanoic acid (3b), which was prepared via condensation of 2-(bromomethyl)furan (10b) with diethyl acetamidomalonate, followed by partial hydrolysis of the resultant diethyl ester (3a) in the presence of barium hydroxide. H...

Treatment of 1-(5-bromo-2-chloro-6-methylpyrimidin-4-yl)-1-methylhydrazine with dimethylthiocarbamoylchloride gave 7-chloro-N,N,1,5-tetramethyl-1H-pyrimido[4,5-e][1,3,4]thiadiazin-3-amine in basic acetonitrile. The latter compounds were reacted with secondary amines in boiling ethanol to afford the related 7-amino derivatives.

Treatment of 1-(5-bromo-2-chloro-6-methylpyrimidin-4-yl)-1-methylhydrazine withdimethylthiocarbamoylchloride gave 7-chloro-N,N, 1,5-tetramethyl-1H-pyrimido[4,5-e][1,3,4]thiadiazin-3-amine in basic acetonitrile. The latter compounds were reacted withsecondary amines in boiling ethanol to afford the related 7-amino derivatives.

P-Silylated N,N-dialkyl amines (5) were easily synthesized in good to excellent yield from aldehydes (1), trimethylsilyldialkylamines (2), and trimethylsilylmethylmagnesium chloride (4) in the presence of 5 M lithium perchlorate solution in diethyl ether. The reaction Of (2) with aldehyde proceeded smoothly in the LiCI0 , to give the imimum salt (3). Addition of trimethylsilylmethylrnagnes...