A new approach for the synthesis of 4-oxo-3-quinolinecarboxylic acid derivatives is described. This methodology involves the C-acylation of the anions of appropriate beta-keto esters with novel N-hydroxysuccinimide esters of anthranilic acids. The intermediate C-acylation products 3 are spontaneously cyclized to afford 3-ethoxycarbonyl-4-oxoquinoline derivatives 4. The introduction of a variety...

Selective acylation of alcohol has enjoyed great attraction of chemists due to its significance in synthetic organic chemistry especially in protecting group chemistry as reflected by the number of methods that have been developed to effect this transformation. To meet the challenging task of chemoselective transformation of aliphatic alcohols in the presence of phenolic alcohol mainly acidic c...

Protein S-acylation (also called palmitoylation) is a pervasive post-translational modification that plays critical roles in regulating protein trafficking, localization, stability, activity, and complex formation. The past decade has witnessed tremendous advances in the study of protein S-acylation, largely owing to the development of novel S-acylproteomics technologies. In this review, we sum...

A palladium-catalyzed decarboxylative C2-acylation of indoles with α-oxocarboxylic acids was achieved. This protocol represents a novel and complementary approach to 2-aroylindoles.

Nano sulfated titania was tested as solid acid heterogeneous catalyst for the synthesis of 4-(Trifluoromethyl) coumarin and coumarin derivatives under solvent-free condition. Factorial design evidenced a positive effect of reaction temperature, amount of catalyst, and solvents.  This nano-sized sulfated titania has been prepared by a sol-gel hydrothermal process. The prepared sulfated titania s...

We wish to report a simple synthetic procedure, which permits the regiospecific mono-acylation, alkylation and silylation at the 2-position of allyl 4,6-O-benzylidene alpha-D-glucopyranoside in high yields and which does not require the use of catalysts.

The major physiological inhibitors of insulin secretion, norepinephrine, somatostatin, galanin, and prostaglandin E2, act via specific receptors that activate pertussis toxin (PTX)-sensitive G proteins. Four inhibitory mechanisms are known: 1) activation of ATP-sensitive K channels and repolarization of the beta-cell; 2) inhibition of L-type Ca2+ channels; 3) decreased activity of adenylyl cycl...

Bacillus subtilisin has been a popular model protein for engineering altered substrate specificity. Although some studies have succeeded in increasing the specificity of subtilisin, they also demonstrate that high specificity is difficult to achieve solely by engineering selective substrate binding. In this paper, we analyze the structure and transient state kinetic behavior of Sbt160, a subtil...

A particulate preparation isolated from Escherichia coli B catalyzes the acylation of 1-acyl-an-glycerol j-phosphate (I-acyl-GP) with both oleoyl-CoA and pahnitoyl-CoA. The optimum conditions were determined for the acyl-CoA: I-acyl-GP acyltransferase. The acyltransferase is specific for the I-acyl-GP and does not acylate 2-acyl-sn-glycerol 3-phosphate (2-acyl-GP) under the conditions used. The...