Synthesis of dendritic bisphosphonates as bone targeting ligands

Autor: Kenta Ueda, Go Hirai, Hiroshi Suemune, Kazuma Shimoda, Mariko Aso, Takahiro Mitsuoka
Rok vydání: 2018
Předmět:
Zdroj: Tetrahedron Letters. 59:4528-4531
ISSN: 0040-4039
Popis: A dendritic bisphosphonate carrying three bisphosphonate (BP) units in close proximity was designed as a ligand to conjugate large therapeutic molecules for their bone selective delivery. The Bu3P-catalyzed conjugate addition of nitromethane to vinylidene bisphosphonate was effective to construct a quaternary carbon center carrying BP units. Owing to multivalent interactions, the dendritic bisphosphonate showed considerable affinity for the bone mineral hydroxyapatite even in the presence of a competitor, demonstrating potential as a bone targeting ligand.
Databáze: OpenAIRE