Oxa-spirocycles: synthesis,properties and applications |
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| Authors: | Kateryna Fominova,Taras Diachuk,Dmitry Granat,Taras Savchuk,Vladyslav Vilchynskyi,Oleksiy Svitlychnyi,Vladyslav Meliantsev,Igor Kovalchuk,Eduard Litskan,Vadym V. Levterov,Valentyn R. Badlo,Ruslan I. Vaskevych,Alla I. Vaskevych,Andrii V. Bolbut,Volodymyr V. Semeno,Rustam Iminov,Kostiantyn Shvydenko,Anastasiia S. Kuznetsova,Yurii V. Dmytriv,Daniil Vysochyn,Vasyl Ripenko,Andrei A. Tolmachev,Olexandra Pavlova,Halyna Kuznietsova,Iryna Pishel,Petro Borysko,Pavel K. Mykhailiuk |
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| Affiliation: | Enamine Ltd, Chervonotkatska 78, 02094 Kyiv Ukraine, .; Institute of Organic Chemistry, National Academy of Sciences of Ukraine, Murmanska St. 5, 02094 Kyiv Ukraine ; National Technical University of Ukraine, Igor Sikorsky Kiev Polytechnic Institute, Prosp. Peremohy 37, 03056 Kyiv Ukraine ; National Research Tomsk Polytechnic University, Lenin Ave. 30, 634050 Tomsk Russia ; Bienta, Chervonotkatska 78, 02094 Kyiv Ukraine, |
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| Abstract: | A general approach to a new generation of spirocyclic molecules – oxa-spirocycles – was developed. The key synthetic step was iodocyclization. More than 150 oxa-spirocyclic compounds were prepared. Incorporation of an oxygen atom into the spirocyclic unit dramatically improved water solubility (by up to 40 times) and lowered lipophilicity. More potent oxa-spirocyclic analogues of antihypertensive drug terazosin were synthesized and studied in vivo.A general practical approach to a new generation of spirocyclic molecules – oxa-spirocycles – is developed. |
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