The use of methanesulfonic acid as a Brønsted acid for direct ortho-acylation of phenols and naphthols proves to be a convenient, more general and direct route to various hydroxyaryl ketones. The route is regioselective, leading to ortho C-acylated products in satisfactory to high yields in most cases. The solvent free reactions described below exhibited environmentally benign in terms of faste...

The use of methanesulfonic acid as a Brønsted acid for direct ortho-acylation of phenols and naphthols proves to be a convenient, more general and direct route to various hydroxyaryl ketones. The route is regioselective, leading to ortho C-acylated products in satisfactory to high yields in most cases. The solvent free reactions described below exhibited environmentally benign in terms of faste...

Key words Prins reaction - Friedel–Crafts acylation piperidine schizophrenia

the use of methanesulfonic acid as a brønsted acid for direct ortho-acylation of phenols and naphthols proves to be a convenient, more general and direct route to various hydroxyaryl ketones. the route is regioselective, leading to ortho c-acylated products in satisfactory to high yields in most cases. the solvent free reactions described below exhibited environmentally benign in terms of faste...

Protein S-acylation is a major posttranslational modification whereby a cysteine thiol is converted to a thioester. A prototype is S-palmitoylation (fatty acylation), in which a protein undergoes acylation with a hydrophobic 16 carbon lipid chain. Although this modification is a well-recognized determinant of protein function and localization, current techniques to study cellular S-acylation ar...

Organocatalytic regioselective acylation of mono- and disaccaharides with various functionalized acid anhydrides has been developed. Acylation of octyl beta-D-glucopyranoside with acid anhydrides derived from alpha-amino acids, cinnamic acid, and gallic acid took place at C(4)-OH with 67-94% regioselectivity in the presence of catalyst 1. Regioselective acylation of disaccharides with functiona...

In conclusion, our results show that inhibitors of acylation may be developed on the basis of analogues of myristic acid. Such inhibitors inhibit not only the N-myristoyl transferase activity, but also acylation of proteins in intact cells. They are also able to inhibit virus acylation. Preliminary results show that they inhibit HIV release from infected H9 cells in culture and therefore may be...

Ras proteins play vital roles in numerous biological processes and Ras mutations are found in many human tumors. Understanding how Ras proteins are regulated is important for elucidating cell signaling pathways and identifying new targets for treating human diseases. Here we report that one of the K-Ras splice variants, K-Ras4a, is subject to lysine fatty acylation, a previously under-studied p...

Protein S-acylation, the reversible covalent fatty-acid modification of cysteine residues, has emerged as a dynamic posttranslational modification (PTM) that controls the diversity, life cycle, and physiological function of numerous ligand- and voltage-gated ion channels. S-acylation is enzymatically mediated by a diverse family of acyltransferases (zDHHCs) and is reversed by acylthioesterases....

2D NMR revealed a correspondence between the molecular structure of lignins and their degree of acylation in several nonwoody angiosperms characterized by different lignin acylation types (acetate and/or p-coumarate esters) and extents (up to more that 90% of units). Some of the lignin substructures identified showed that acylation is produced at the monolignol level. Direct evidence was also p...