Oxa-spirocycles: synthesis, properties and applications

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 u...

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Detalles Bibliográficos
Autores principales: Fominova, Kateryna, Diachuk, Taras, Granat, Dmitry, Savchuk, Taras, Vilchynskyi, Vladyslav, Svitlychnyi, Oleksiy, Meliantsev, Vladyslav, Kovalchuk, Igor, Litskan, Eduard, Levterov, Vadym V., Badlo, Valentyn R., Vaskevych, Ruslan I., Vaskevych, Alla I., Bolbut, Andrii V., Semeno, Volodymyr V., Iminov, Rustam, Shvydenko, Kostiantyn, Kuznetsova, Anastasiia S., Dmytriv, Yurii V., Vysochyn, Daniil, Ripenko, Vasyl, Tolmachev, Andrei A., Pavlova, Olexandra, Kuznietsova, Halyna, Pishel, Iryna, Borysko, Petro, Mykhailiuk, Pavel K.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2021
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8447932/
https://www.ncbi.nlm.nih.gov/pubmed/34667540
http://dx.doi.org/10.1039/d1sc03615g
Descripción
Sumario: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.

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