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Information × Registration Number 0212U008738, 0112U006062 , R & D reports Title The development of new approaches to the synthesis of medium azacycles annulated with aryl (hetaryl) fragment popup.stage_title Head Tolkunov Sergey Volodimir, Registration Date 26-12-2012 Organization The L.M.Litvinenko Institute of Physical-Organic Chemistry and Coal Chemistry popup.description2 Object of research - medium azacycles annulated with aryl (hetaryl) fragment, which contain heteroatoms of oxygen, nitrogen and sulfur. The purpose of work - development of methods of synthesis and updating of structures tetrahydrobenzothieno[2,3-c]azepines, azicines, thienо[2,3:5',4']thieno[2,3-с]pyridines by use of Pictet-Spengler reaction. Metods of research - methods of organic synthesis, mass- and NMR - spectroscopy. Cyclization of benzothienyl-3-propylamines in conditions of Pictet-Spengler reaction is investigated. New derivatives of tetrahydrobenzothieno[2,3-c]azepines was synthesized. The methods of synthesis of 4-bromolevulinic acid esters and 2-bromolevulinic ester based on bromation of levulinic acid in methanol media are developed. Benzo[b]thieno-3-propionic acids and benzofuran-3-propionic acid obtained by cyclization of phenylmercaptolevulinic or phenoxylevulinic esters in polyphosphoric acid. The methods of synthesis of 3-methylbenzothieno-2-acetic acid by cyclization of phenylmercaptolevulinic esters in polyphosphoric acid are developed. Benzothienoazepines and benzofuroazepines obtained by cyclization hetarylpropylamines in Pictet-Spengler and Eschweiler-Clarc reactions. A new strategy for the synthesis of the eight-membered heterocyclic skeleton of benzothieno[2',3':4,5][1,2]diazocino[8,1-b]quinazolin-9-оnes, based on the Pictet-Spengler reaction of 3-amino-2-[2-(benzothienyl-3)ethyl]quinazolin-4(3H)-one with carbonyl compounds in acidic media, is proposed. The results of work can be utilised in organic chemistry, for synthesis of biologically active compounds, for creation of new drugs. Product Description popup.authors Ереско О.Б. Тамаркина Ю.В. Толкунов В.С. popup.nrat_date 2020-04-02 Close