1373028-07-9Relevant academic research and scientific papers
Oxa-spirocycles: synthesis, properties and applications
Badlo, Valentyn R.,Bolbut, Andrii V.,Borysko, Petro,Diachuk, Taras,Dmytriv, Yurii V.,Fominova, Kateryna,Granat, Dmitry,Iminov, Rustam,Kovalchuk, Igor,Kuznetsova, Anastasiia S.,Kuznietsova, Halyna,Levterov, Vadym V.,Litskan, Eduard,Meliantsev, Vladyslav,Mykhailiuk, Pavel K.,Pavlova, Olexandra,Pishel, Iryna,Ripenko, Vasyl,Savchuk, Taras,Semeno, Volodymyr V.,Shvydenko, Kostiantyn,Svitlychnyi, Oleksiy,Tolmachev, Andrei A.,Vaskevych, Alla I.,Vaskevych, Ruslan I.,Vilchynskyi, Vladyslav,Vysochyn, Daniil
, p. 11294 - 11305 (2021)
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 studiedin vivo.
