We report copper-catalyzed oxidative dehydrogenative carboxylation (ODC) of unactivated alkanes with various substituted benzoic acids to produce the corresponding allylic esters. Spectroscopic studies (EPR, UV-vis) revealed that the resting state of the catalyst is [(BPI)Cu(O2CPh)] (1-O2CPh), formed from [(BPI)Cu(PPh3)2], oxidant, and benzoic acid. Catalytic and stoichiometric reactions of 1-O...

Direct and atom-economical amidation of nonsteroidal anti-inflammatory drugs naproxen ibuprofen ketoprofen with a variety secondary amines was effected using commercially available DCC under mild open-air conditions. These prodrug amides were obtained in good to moderate yields ranging between 30–90 %.

Amides are important structural motifs in pharmaceutical and agrochemical chemistry because of the intriguing biological active properties. We report here amidation commercially available es...

Highly efficient method for the preparation of N-tert-butyl amides by reaction of nitriles with tertbutylacetateis described using boron trifluoride etherate in solvent free condition. Selective amidation ofbenzonitrile in the presence of acetonitrile was also achieved.

We approach chemical synthesis by identifying biomedically interesting natural products that offer an opportunity for methodology development. Thus, a potential target is subject to extensive retrosynthetic analysis to evaluate possible routes. This may reveal that a yet unknown reaction would facilitate the synthetic problem. Suitable methodology is then developed and ultimately applied to the...

Mechanisms underlying the specificity and efficiency of enzymes, which modify peptide messengers, especially with the variable requirements of synthesis in the neuronal secretory pathway, are poorly understood. Here, we examine the process of peptide alpha-amidation in individually identifiable Lymnaea neurons that synthesize multiple proproteins, yielding complex mixtures of structurally diver...

Present on archaeal and eukaryotic translation elongation factor 2, diphthamide represents one of the most intriguing post-translational modifications on proteins. The biosynthesis of diphthamide was proposed to occur in three steps requiring seven proteins, Dph1-7, in eukaryotes. The functional assignments of Dph1-5 in the first and second step have been well established. Recent studies sugges...

Exocrine secretion granules from the rat parotid gland contain a carboxyl-terminal peptide alpha-amidation enzyme resembling closely an enzyme from the pituitary (peptidyl-glycine alpha-amidating monooxygenase) that functions in post-translational processing of secretory polypeptides within neural and endocrine secretion granules. alpha-Amidation is a characteristic (often essential) chemical f...

In many prokaryotes and in organelles asparagine and glutamine are formed by a tRNA-dependent amidotransferase (AdT) that catalyzes amidation of aspartate and glutamate, respectively, mischarged on tRNAAsn and tRNAGln. These pathways supply the deficiency of the organism in asparaginyl- and glutaminyl-tRNA synthtetases and provide the translational machinery with Asn-tRNAAsn and Gln-tRNAGln. So...