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Information × Registration Number 0224U033146, (0124U002052) , R & D reports Title Creation of fluorine- and phosphorus-containing building blocks, including optically active ones, for the needs of medical chemistry and agrochemistry popup.stage_title Конструювання С-С та С-Р зв'язку біля азометинового вуглецю N-(трет-бутилсульфініл)поліфтороалкілімінів Head Cherednichenko Alona S., Доктор філософії Registration Date 19-12-2024 Organization Institute of Organic Chemistry NAS of Ukraine popup.description1 The purpose of the project is the synthesis of new, in particular enantiomerically pure, fluorine-containing acyclic and heterocyclic systems, including those modified with a phosphine oxide fragment - valuable objects for medical chemistry. In the course of the scientific research, two strategies are planned for obtaining fluorine-containing structures - direct fluorination using safe N-F-reagents and synthesis using ready-made fluorine-containing building blocks. popup.description2  As a result of the 1st stage of the scientific project, a number of fluorine-containing compounds capable of further functional modification have been obtained. An effective and scalable method of asymmetric synthesis of universal aminoalkyldimethylphosphine oxide derivatives has been developed, which consists in the three-component reaction of enantiomeric Ellman amides, aldehydes and dimethylphosphine oxide in the presence of titanium tetraisopropylate. A convenient preparative approach to a number of functionalized dimethylphosphinoyl-containing cyclopropanes and cyclobutanes has been developed, the basis of which is the cyclocondensation of dimethylphosphinoylacetonitrile with 1,2- and 1,3-dibromoalkanes. On the basis of the developed procedure, synthetic procedures have been developed for obtaining nitriles, amines and carboxylic acids, which combine in their structure popular in drug design small saturated cyclic systems of cyclopropane or cyclobutane and a dimethylphosphine oxide fragment. An effective scaled method for the synthesis of all isomeric pyridinyl oxoacetates has been developed, based on the interaction of the corresponding bromopyridines with diethyloxalate in the presence of isopropylmagnesium chloride. By deoxofluorination of pyridinyl oxoacetates with sulfur tetrafluoride, all isomeric pyridinyl difluoroacetate esters and all isomeric pyridinyltetrafluorinated ethers have been obtained. A series of polyfluoroalkylamino esters have been obtained by the interaction of N-tert-butylsulfenylimine trifluoropyruvate with a number of alkyl and aryl organomagnesium compounds, from which a number of biologically promising enantiomerically pure polyfluoroalkylamino acids, amino alcohols and 3,3-heme-substituted polyfluoroalkyl-containing NH-morpholines. Product Description popup.authors Aleksandrova Anastasiia M. Shavrina Oksana M. popup.nrat_date 2024-12-19 Close