Heterocyclization Reactions of Pyruvic Acids and Aminoazoles with Controlled Chemoselectivity

The present review includes the analysis of known literature data concerning linear and multicomponent heterocyclizations involving pyruvic acids and aminoazoles. In particular, the review demonstrates the approaches to control regio- and chemoselectivity of these types of treatments and their application to solve the matters of Diversity Oriented Synthesis

STUDY OF THE PROPERTIES OF MARSHMALLOW WITH THE SUDANESE ROSE AND BLACK CHOKEBERRY DYES UPON STORAGE

Creation of marshmallow with natural dyes is impossible without investigation of properties of products and estimation of its quality. Our objects of investigation were organoleptic, physico-chemical and antioxidant properties of the products at storage for 30 days. The six of marshmallow samples were the objects of our research. They differed in the type of structuring agent - gelatin or gelatin with solubilized substances and the type of dye – water or water-alcohol extract of cryopowder from Sudanese rose or water-alcohol extract of cryopowder from вlack chokeberry. Necessary indexes of quality are supplied for the new types of marshmallow with natural dyes. Moisture content (19.0 ... 21.5 %), total acidity (3.5 °Brix), density (0.51 ... 0.67 g/cm3), reducing substances content (not more than 13.6 %) were determined by standard methods. Use of natural anthocyanin dyes let us to increase antioxidant properties of the ready product. Value of antioxidant capacity of the new samples, determined with use of galvanostatic coulometry method, is in 2 ... 2.5 times more than the same results for samples, made without the dyes. It was established that short time storage (up to 2 days) of marshmallow with natural anthocyanin dyes at temperature (15...18)°С and relative air humidity 60...75 % is possible without packing materials. Storage of the products in hermetically polyethylene wrap and cardboard box provides high indexes of quality, stability of colour in long time (up to 30 days). It was shown that antioxidant properties of marshmallow with water-alcohol extracts of cryopowder from Sudanese rose and black chokeberry remain stable. The new developed types of marshmallow with natural anthocyanin dyes makes wide market of confectionery and can be used for correction of feeding of a man

Doebner-type pyrazolopyridine carboxylic acids in an Ugi four-component reaction

Substituted 1H-pyrazolo[3,4-b]pyridine-4- and 1H-pyrazolo[3,4-b]pyridine-6-carboxamides have been synthetized through a Doebner–Ugi multicomponent reaction sequence in a convergent and versatile manner using diversity generation strategies: combination of two multicomponent reactions and conditions-based divergence strategy. The target products contain as pharmacophores pyrazolopyridine and peptidomimetic moieties with four points of diversity introduced from readily available starting materials including scaffold diversity. A small focused compound library of 23 Ugi products was created and screened for antibacterial activity

Aminoazole-Based Diversity-Oriented Synthesis of Heterocycles

The comprehensive review contains the analysis of literature data concerning reactions of heterocyclization of aminoazoles and demonstrates the application of these types of transformations in diversity-oriented synthesis. The review is oriented to wide range of chemists working in the field of organic synthesis and both experimental and theoretical studies of nitrogen-containing heterocycles

The Groebke-Blackburn-Bienayme Reaction

Imidazo[1,2a]pyridine is a well‐known scaffold in many marketed drugs, such as Zolpidem, Minodronic acid, Miroprofen and DS‐1 and it also serves as a broadly applied pharmacophore in drug discovery. The scaffold revoked a wave of interest when Groebke, Blackburn and Bienaymé reported independently a new three component reaction resulting in compounds with the imidazo[1,2‐a]‐heterocycles as a core structure. During the course of two decades the Groebke Blackburn Bienaymé (GBB‐3CR) reaction has emerged as a very important multicomponent reaction (MCR), resulting in over a hundred patents and a great number of publications in various fields of interest. Now two compounds derived from GBB‐3CR chemistry received FDA approval. To celebrate the first 20 years of GBB‐chemistry , we present an overview of the chemistry of the GBB‐3CR, including an analysis of each of the three starting material classes, solvents and catalysts. Additionally, a list of patents and their applications and a more in‐depth summary of the biological targets that were addressed, including structural biology analysis, is given

Evaluation of the Oxidative Stability of Emulsifiers of an Acylglicerol Origin

Obtaining new environmentally friendly emulsifiers of an acylglycerol origin based on sunflower oil with unsaturated fatty acids that are harmless to human health is relevant. The authors of this study obtained such emulsifiers under mild conditions (35–40 °C) by the transesterification reaction of triacylglycerols obtained from sunflower oil. Changes in the UV spectra of 0.02% solutions in isooctane were studied in the range from 200 to 285 nm depending on the storage duration and storage temperature of the emulsifiers and oils. The results showed that, in the process of storage, the new emulsifiers showed a higher resistance to oxidation compared to oil