The upscaling of biphasic photochemical reactions is challenging because of the inherent constraints of liquid-gas mixing and light penetration. Using semi-permeable coaxial flow chemistry within a modular photoreactor, the photooxidation of the platform chemical furfural was scaled up to produce routinely 29 gram per day of biobased building block hydroxybutenolide, a precursor to acrylate alternatives.
Inhibition of the sodium−glucose cotransporter 2 (SGLT2) by canagliflozin in type 2 diabetes mellitus results in large between-patient variability in clinical response. To better understand this variability, the positron emission tomography (PET) tracer [18F]canagliflozin was developed via a Cu-mediated 18F-fluorination of its boronic ester precursor with a radiochemical yield of 2.0 ± 1.9% and a purity of >95%. The GMP automated synthesis originated [18F]canagliflozin with a yield of 0.5−3% (n = 4) and a purity of >95%. Autoradiography showed [18F]canagliflozin binding in human kidney sections containing SGLT2. Since [18F]canagliflozin is the isotopologue of the extensively characterized drug canagliflozin and thus shares its toxicological and pharmacological characteristics, it enables its immediate use in patients.
