3,3-difluorooxetane: Gram level synthesis revealed

3,3-difluorooxetane: Gram level synthesis revealed



Oxycyclobutane itself is unstable and prone to ring opening under acidic or high-temperature conditions; It is generally believed that the 3,3-disubstitution on its ring can stabilize the small ring skeleton. The introduction of fluorine atoms is generally believed to have a significant impact on the spatial orientation and physicochemical properties of molecular structures. Therefore, 3,3-difluorooxetane, as a functional group for bioelectronic isostructural iteration, has important applications in drug discovery.
Recently, Enamine, a renowned international molecular block company, announced in Chem A research article was published in Eur. J. journal, introducing the gram level synthesis of 3,3-difluorooxetane block molecules,
Quantification of steric hindrance and electronic properties, determination of physicochemical properties (pKa, LogP), and chemical stability.
The biological evaluation of bioelectronic isotopes as drug candidate molecules revealed the application of 3,3-difluorooxetane (3,3-diFOx) fragments in early drug discovery.


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