A novel method for the mono-N-alkylation of primary amines, diamines, and polyamines was developed using cesium bases in order to prepare secondary amines efficiently. A cesium base not only promoted alkylation of primary amines but also suppressed overalkylations of the produced secondary amines. Various amines, alkyl bromides, and alkyl sulfonates were examined, and the results demonstrated t...

Excited-state palladium catalysis is an efficient process for the alkylation of diverse organic compounds via generation alkyl radicals from bromides and iodides. However, more stable chlorides remains challenging. Herein, we demonstrate excited-state palladium-catalyzed synthesis oxindoles isoquinolinediones alkylation/annulation reaction by overcoming inherent limitations associated with unac...

Alkylation is a very important chemical reaction which modifies the biological properties of drugs. Quinazolinedione derivatives are of considerable interest due to their wide array of pharmacological properties.We now report application of a practical alkylation procedure to several quinazolinediones, including pelanserine (5f), which shows antihypertensive properties, 1-methyl-3-(2'-phenyleth...

Heme alkylation by the antimalarial drug artemisinin is reported in vivo, within infected mice that have been treated at pharmacologically relevant doses. Adducts resulting from the alkylation of heme by the drug were characterized in the spleen of treated mice, and their glucuroconjugated derivatives were present in the urine. Because these heme-artemisinin adducts were not observed in noninfe...

A general method for intermolecular allylic C-H alkylation of terminal olefins with tertiary nucleophiles has been accomplished employing palladium(II)/bis(sulfoxide) catalysis. Allylic C-H alkylation furnishes products in good yields (avg. 64%) with excellent regio- and stereoselectivity (>20:1 linear:branched, >20:1 E:Z). For the first time, the olefin scope encompasses unactivated aliphatic ...

The covalent sequence specificity of a series of nitrogen mustard and imidazole-containing analogues of distamycin was determined using modified sequencing techniques. The analogues tether benzoic acid mustard (BAM) and possess either one, two or three imidazole units. Examination of the alkylation specificity revealed that BAM produced guanine-N7 lesions in a pattern similar to conventional ni...

Mitomycin C (MC) activation to a reactive species was studied in nuclei isolated from rat liver and EMT6 tumor cells. Both preparations were similar in the rate of 4-(p-nitrobenzyl)pyridine (NBP) alkylation by MC and the levels of NADPH-cytochrome P-450 reductase. MC activation by both hepatic and EMT6 cell nuclei was inhibited by the presence of O2 and by heat inactivation. NADPH was preferred...

Ethyl benzene used increasingly each year is the raw material of producing styrene monomer. This substanceis produced from benzene alkylation with ethylene or ethanol, depending on the availability and cost of rawmaterials. In this study benzene alkylation in the presence of ethanol in a catalytic fixed bed reactor inthree states of isotherm, adiabatic and non-isotherm-non-adiabatic is mathemat...

ethyl benzene used increasingly each year is the raw material of producing styrene monomer. this substanceis produced from benzene alkylation with ethylene or ethanol, depending on the availability and cost of rawmaterials. in this study benzene alkylation in the presence of ethanol in a catalytic fixed bed reactor inthree states of isotherm, adiabatic and non-isotherm-non-adiabatic is mathemat...