Alkylmalonic esters, which have been recognized as important intermediates in the syntheses of various carboxylic acids, amino acids, etc., can be obtained by a variety of methods.1) Excepting the introduction of tertiary alkyl groups, the alkylation of malonic esters with alkyl halides in basic conditions, for example, in ethanol in the presence of sodium ethoxide, is one of the most important...

Antisense oligodeoxyribonucleotides (15mers), containing a 2-(N-iodoacetylaminoethyl)thio-adenine, were synthesized and tested for their ability to cleave complementary DNAs (21mers). Cleavage of the target DNAs was done by alkylation followed by treatment with piperidine, and the positions of the alkylated sites were estimated by identification of the cleaved products. By using several combina...

The in vivo alkylation of DNA by N-nitrosomethyl-(2-hydroxyethyl)amine (NMHEA) was examined in male and female F-344/N rats. NMHEA is a strong hepatocarcinogen in female rats when administered by gavage but a weaker hepatocarcinogen in male rats. Groups of 5 rats of each sex were treated by gavage with various doses of NMHEA dissolved in corn oil. After 4 h the animals were sacrificed and the l...

A method for the preparation of chiral β-aminophosphines having substituted P-aryl groups is described. Ring-opening of cyclic sulfamidates with metal diarylphosphinites yields β-aminophosphine oxides, which are then reduced to the corresponding phosphines. Effects of the diarylphosphinite countercation on the regioselectivity of the ring-opening reaction (P- versus O-alkylation) are discussed....

The direct and regioselective N-alkylation of amino-azoles to the corresponding 2-N-(alkylamino)azoles using various alcohols as alkylating agents with good to excellent yields has been accomplished by an iridium complex/base system.

A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R)-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described.

We report an efficient, highly selective modification on the N-terminal amines of peptides and proteins using aldehyde derivatives via reductive alkylation. After modification of a library of unprotected peptides XYSKEASAL (X varies over 20 natural amino acids) by benzaldehyde at room temperature, pH 6.1 resulted in excellent N-terminal selectivity (α-amino/ε-amino: >99 : 1) and high reaction c...

Alkylation of biphenyl with 1-octene was investigated using ((Al+C3H7Cl)+C2H4) catalysts. The catalytic activity of ((Al+C3H7Cl)+C2H4) for the alkylation was studied at different temperatures, mol ratios of biphenyl to 1-octene, reaction times and catalyst concentrations. It was shown that using this catalyst has more advantagous than another catalysts. Experiments show that by increasing t...

alkylation of biphenyl with 1-octene was investigated using ((al+c3h7cl)+c2h4) catalysts. the catalytic activity of ((al+c3h7cl)+c2h4) for the alkylation was studied at different temperatures, mol ratios of biphenyl to 1-octene, reaction times and catalyst concentrations. it was shown that using this catalyst has more advantagous than another catalysts. experiments show that by increasing tempe...