PEGylation is a well-established technique utilized to overcome the problems related to the therapeutic applications of peptides and proteins. Reasons for the PEGylation of these biological macromolecules include reducing immunogenicity, proteolytic degradation and rapid clearance from blood circulation. Octreotide is an octapeptide analogue of naturally-occurred somatostatin. This peptide has ...

PEGylation is a well-established technique utilized to overcome the problems related to the therapeutic applications of peptides and proteins. Reasons for the PEGylation of these biological macromolecules include reducing immunogenicity, proteolytic degradation and rapid clearance from blood circulation. Octreotide is an octapeptide analogue of naturally-occurred somatostatin. This peptide has ...

In order to study the effect of halogen bond on tautomerism in β-diketones solid-state, we have prepared a series cocrystals derived from an asymmetric β-diketone, benzoyl-4-pyridoylmethane (b4pm), as acceptor and perfluorinated iodobenzenes: iodopentaflourobenzene (ipfb), 1,2-, 1,3- 1,4-diiodotetraflorobenzene (12tfib, 13tfib 14tfib) 1,3,5-triiodo-2,4,6-trifluorobenzene (135titfb). All five ar...

Acylation reaction of a variety of cyclic ketones via acylation of the corresponding enamines is welldefined in the literature. Enamine acylation of carbonyl compounds is a significant synthetic method because of its mildness and the ease of preparing various β-diketones [1-4]. Acylation reactions are performed by means of converting enamines to the enaminoketones and subsequent hydrolysis of t...

A general and simple procedure to access chiral β'-amino-α,β-enones, in seven steps, from an α,β unsaturated ester has been described. The use of a Horner-Wadsworth-Emmons reaction as a key step for generating the β'-amino-α,β-enones, permits access to a range of substrates under mild conditions and in moderate to high yield.

Regioand stereoselective reductions of several diketones to afford enantiopure hydroxy ketones or diols were accomplished using isolated alcohol dehydrogenases (ADHs). Results could be rationalised taking into account different (promiscuous) substrate-binding modes in the active site of the enzyme. Furthermore, interesting natural cyclic diketones were also reduced with high regioand stereosele...

A one-pot synthesis of new variously substituted γ-chloro-γ, β-allylic carbamates have been carried out starting from β-chloro-α, β-unsaturated aldehydes. The and the corresponding intermediates, alcohols, were fully characterized by (1H 13C) NMR, IR HRMS spectroscopic techniques. crystal structures two allylic carbamates, established single-crystal X-ray diffraction.