Precision deuteration at metabolically vulnerable sites of pharmaceuticals can enhance drug stability and therapeutic efficacy, yet existing methods often suffer from poor selectivity and inefficiency.
An efficient and practical bromination/dehydrogenation of tetrahydroquinolines was developed for the one-pot construction of polybromoquinolines under mild conditions. NBS not only acts as an electrophile, but also as an oxidant in this reaction.
A new three-step mechano-synthesis method starts with 4-bromoquinoline, uses Suzuki–Miyaura, Minisci C–H alkylation, and oxidation Heck coupling reactions, leading to rapid and eco-friendly synthesis of the key Pitavastatin intermediate.
A novel oxo-bridged CuNiO2 nanocatalyst is reported for the first time, enabled water-mediated Csp2–S cross-coupling with a broad substrate scope and gram-scale synthesis of challenging heteroaryl thioethers, including bioactive motifs.
Synthesis and biological testing of the R- and S-enantiomers of LW223, a third generation TSPO PET imaging agent using human brain tissue showed that despite a 7.5-fold difference in affinity, both are insensitive to rs6971 polymorphism.