At radiolabeled APBA-FAPI for enhanced targeted-alpha therapy of glioma.

Fibroblast activation protein-α (FAPα) is highly expressed in tumor-associated cells and has become one of the most attractive targeting sites in cancer diagnosis and therapy. To ameliorate the rapid metabolism of FAPα inhibitor (FAPI), here, a multifunctional binding agent was introduced to simultaneously achieve At radiolabeling and tumor retention prolongation of corresponding radiolabeled drug. At-APBA-FAPI was successfully synthesized by conjugating At with the designed FAPI carrier in satisfactory radiochemical yield (>60 %).

Total Synthesis of Vilmoraconitine.

Vilmoraconitine belongs to one of the most complex skeleton types in the C-diterpenoid alkaloids, which architecturally features an unprecedented heptacyclic core possessing a rigid cyclopropane unit. Here, we report the first total synthesis of vilmoraconitine relying on strategic use of efficient ring-forming reactions. Key steps include an oxidative dearomatization-induced Diels-Alder cycloaddition, a hydrodealkenylative fragmentation/Mannich sequence, and an intramolecular Diels-Alder cycloaddition.

Visible-Light-Induced Dehydrogenative Imidoylation of Imidazo[1,2-]pyridines with α-Amino Acid Derivatives and α-Amino Ketones.

A new and efficient visible-light-promoted dehydrogenative cross-coupling reaction of imidazo[1,2-]pyridines with α-amino carbonyl compounds toward imidoyl imidazo[1,2-]pyridines is developed. A diverse range of imidazo[1,2-]pyridines undergoes the dehydrogenative imidoylation smoothly with α-amino carbonyl compounds to access the corresponding products in satisfactory yields. We have also proposed the possible reaction mechanism based on preliminary mechanistic studies.

Cobalt-Catalyzed Oxidative Phosphonylation of α-Amino Acid Derivatives and α-Amino Ketones for α-Aminophosphonates.

A novel and efficient direct oxidative phosphonylation of α-amino ketones and α-amino acid derivatives with dialkyl phosphites by the catalysis of a cobalt salt under air is disclosed. A variety of α-amino ketones and α-amino acid derivatives underwent the reaction well with dialkyl phosphites to produce the desired α-aminophosphonates. This protocol not only provides an alternative synthetic route for the preparation of diverse α-aminophosphonates but also avoids the use of potentially explosive peroxide agents.