quercetin, a ubiquitous flavonol, represents a promising leading drug for development of new chemotherapeutic agents. however, its limited cytotoxicity to cancer cells hampers its clinical use. in order to obtain novel quercetin derivatives with superior cytotoxicity, seven alkylated quercetin derivatives were synthesized. solubility of these derivatives was determined by turbidimetry. cytotoxi...

alpha-Diphenylphosphinoyl ketones are selectively and sequentially alkylated at the alpha-position. Double lithiation and selective alkylation occurs at the less stabilised gamma-position. Dephosphinoylation of the alkylation products gives ketones. Mono-alkylation is selective, highly crystalline intermediates are formed and a one-pot strategy is possible. The method is ideally suited for the ...

2,6-diaminopyridine is extensively used as a pharmaceutical intermediate and a hair dye coupler as oxidation formulations. it is soluble in protic solvents. primary and secondary amines are n-methylated by various methods such as direct alkylation of amines with hofmann mechanism, but in many of these methods due to overalkylations, we earn a mixture of amino products. consequently, they aren't...

2,6-diaminopyridine is extensively used as a pharmaceutical intermediate and a hair dye coupler as oxidation formulations. It is soluble in protic solvents. Primary and secondary amines are N-methylated by various methods such as direct alkylation of amines with Hofmann mechanism, but in many of these methods due to overalkylations, we earn a mixture of amino products. Consequently, they aren't...

Quercetin, a ubiquitous flavonol, represents a promising leading drug for development of new chemotherapeutic agents. However, its limited cytotoxicity to cancer cells hampers its clinical use. In order to obtain novel quercetin derivatives with superior cytotoxicity, seven alkylated quercetin derivatives were synthesized. Solubility of these derivatives was determined by turbidimetry. Cytotoxi...

A concise synthetic strategy has been developed for the synthesis of the macrolactone core 2 of a unique polyketide callyspongiolide 1. The key features of the strategy included an Evan's asymmetric alkylation, diastereoselective Michael type alkylation, Brown's asymmetric allylation reaction, an allylic alkylation of an activated Z-allylic alcohol and an intramolecular Z-selective intramolecul...

We report N-iodosuccinimide as the most efficient and selective precatalyst among N-halosuccinimides for dehydrative O-alkylation reactions between various alcohols under high-substrate concentration reaction conditions. The protocol is non-metal, one-pot, selective, easily scalable, with excellent yields; enhancing green chemical profiles of these transformations.

The intermolecular interactions of metallothionein with nitrogen mustard drugs were studied by molecular dynamics simulations. Previous laboratory experiments have defined selective alkylation of two cysteine residues, and selective binding was proposed to precede alkylation. The present study provides information about accessibility to cysteines based on evaluating the intermolecular energies ...

Kinetic analysis was used as a tool for rational optimization of catalytic direct substitution alcohols to enable selective formation ethers, thioethers, and Friedel–Crafts alkylation products using moisture-tolerant commercially available Zr complex.