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Information × Registration Number 0211U009320, 0111U008360 , 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 14-11-2011 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 benzofurodiazepines, benzothienodiazepines and indolodiazepines including with use of Bischler-Napieralsky and Pictet-Spengler reaction. Metods of research - methods of organic synthesis, mass- and NMR - spectroscopy, X-ray analysis. The methods of synthesis of benzofurodiazepines, benzothienodiazepines and indolodiazepines by ring formation derivative of 2-aroylbenzothieno -3-, 2- aroylbenzofuro-3- and 2- aroylindolo- 3-acetic acids by hydrazine hydrate in various experimental conditions are developed. In contrast to 2-aroylbenzene derivative 2-acetylbenzothieno-3-acetyc acid react with hydrazine with reception hydrozones, which in conditions of acid catalysis interacted to 2-amino-1-methylbenzothieno[2,3-с]pyridines. The chemical updating of structure 3,5-dihydro-4H-[1]benzofuro [2,3-d][1,2]diazepin-4-оne and 3,5 dihydro-4H-[1] benzofuro[2,3-d][1,2]diazepin-4-thione is carried out. A number new derivative of 3-N-substituted benzofuro[2,3-d][1,2]diazepines are obtained. The direct conversion benzofuro[2,3-d][1,2]diazepin-4-ones is carried out in benzofuro[3,2-e][1,2,4]triazolo[4,3-b][1,2]diazepines by method of silylation-amination. The new method of synthesis unknown 9-(4-chlorophenyl)-3-methyl-6-phenyl-6,12-dihydro-7H-benzofuro[3,2-e][1,2,4]triazolo[4,3-b][1,2]diazepines based on interaction 4-aminotriazole with aromatic aldehydes in conditions of Pictet-Spengler reaction is developed. 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. Земская Е.О. Толкунов В.С. Хижан О.І popup.nrat_date 2020-04-02 Close