COMBINED METHOD OF OBTAINING PHOSPHORYLATED MONO- AND DIIMIDATES

The interaction of mono- and diimidate hydrochlorides with dialkyl chlorophosphates in the presence of triethylamine without the release of free imidates was studied. A combined method for obtaining N-phosphorylated derivatives of imidic acids with potential biological activity has been developed.

Biosynthesis of D-Mannitol by Diplodia pinea

Research with fungi in search of substances with potential biological activity is gaining more prominence since they are sustainable sources of new molecules. Diplodia pinea is a phytopathogenic fungus found in forest species, which has shown few reports of molecules with biological activity and may present promising biotechnological potential. Thus, the objective of this study was to detect substances produced by this fungus in a liquid medium, under stressful conditions. A metabolite was detected in the alcoholic fraction characterized by X-ray diffraction as D-mannitol. This is the first description of this monosaccharide produced by D. pinea.

Synthesis of α-Aminophosphonates and Related Derivatives; The Last Decade of the Kabachnik–Fields Reaction

The Kabachnik–Fields reaction, comprising the condensation of an amine, oxo compound and a P-reagent (generally a >P(O)H species or trialkyl phosphite), still attracts interest due to the challenging synthetic procedures and the potential biological activity of the resulting α-aminophosphonic derivatives. Following the success of the first part (Molecules 2012, 17, 12821), here we summarize the synthetic developments in this field accumulated in the last decade. The procedures compiled include catalytic accomplishments as well as catalyst-free and/or solvent-free “greener” protocols. The products embrace α-aminophosphonates, α-aminophosphinates, and α-aminophosphine oxides along with different bis derivatives from the double phospha-Mannich approach. The newer developments of the aza-Pudovik reactions are also included.

A Stereoselective, Multicomponent Catalytic Carbonylative Approach to a New Class of α,β-Unsaturated γ-Lactam Derivatives

We report a stereoselective, multicomponent catalytic carbonylative approach to a new class of α,β-unsaturated γ-lactam derivatives with potential biological activity, that are, alkyl (Z)-2-(2-oxopyrrolidin-3-ylidene)acetates. Our method is based on the catalytic assembly of readily available building blocks, namely, homopropargylic amines, carbon monoxide, an alcohol, and oxygen (from air). These simple substrates are efficiently activated in ordered sequence under the action of a very simple catalytic system, consisting of PdI2 in conjunction with KI to give the γ-lactam products in 47–85% yields. Carbonylation reactions are carried out at 100 °C for 2–5 h under 40 atm of a 4:1 mixture of CO‒air, with 0.5–5 mol% of PdI2 and 5–50 mol% of KI.

Recent advances of N-heterocyclic carbenes in the applications of constructing carbo- and heterocyclic frameworks with potential biological activity

A general picture of utilization of NHCs in constructing several kinds of bioactive cyclic skeletons.

Derivatives of 1,2,4-Triazole-3,4-Disubstituted Based on Aminoacids with Potential Biological Activity

In order to obtain new substances with potential biological activity dipeptide derivatives from p-aminobenzoyl-phenylglycine and p-aminobenzoyl-phenylalanine were grafted on 1,2,4-triazolic heterocycle. The new synthesized compounds belong to the group of antimetabolites, group used in medicine for treating malignant tumors. Also, it is possible to study the correlation between chemical structure and biological activity of the new compounds.