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Information × Registration Number 0219U102157, 0114U003956 , R & D reports Title Development of approaches to the synthesis of polyfunctional conformationally restricted amine derivatives for medicinal and agro chemistry popup.stage_title Head Volochnyuk Dmytro M., Доктор хімічних наук Registration Date 20-12-2019 Organization Institute of Organic Chemistry NAS of Ukraine popup.description2  A general strategy for the design of lead-like compound libraries for pharmaceutical and agrochemical industry is proposed. The key steps in achieving this goal were the theoretical study of the lead-like chemical space and detection of "white spots" in it, the development of effective synthetic approaches to obtain building blocks and parallel synthesis procedures using such blocks to fill the "white spots" with really existing chemical compounds. The synthesis methodology was developed and the properties of spiro [3.3] heptane derivatives functionalized in 1,6- and 2,6-positions were studied, which allowed to obtain all stereoisomers of orthogonally protected spiro[3.3]heptane-1,6-diamines and fluorinated spiro[3.3]heptanes and azaspiro[3.3]heptanes. A preparative strategy for the synthesis of gem-difluorocycloalkanes with the ring size C4 – C6 containing various functional groups (-COOH, NH2, CH2NH2, CH=OH, Br, SO=Cl, BPin) has been developed. An effective strategy for the synthesis of C-(cyclo)alkyl substituted pyridines and piperidines was found. Difluorocyclopropanation of functionalized electron-rich and electron-deficient alkenes with the TMSCF3 - NaI system under the conditions of "slow addition" protocol was studied. On the basis of this reaction, a methodology for the preparative synthesis of functionalized difluorocyclopropanes was developed, and the limitations of its application were found. The tolerance of the difluorocyclopropane fragment to a number of basic transformations of organic chemistry was studied. Product Description popup.authors Ivonin Sergiy P. Gorlova Alina O. Zarudnitskii Evgenij V. Kurpil’ Bogdan B. Melnykov Kostyantin P. Nosik Pavlo S. Sibgatulin Dmytro O. Slobodyanyuk Evgeniy Yu. Subota Andrij I. Chernykh Anton V. popup.nrat_date 2020-04-02 Close