Author/Authors :
Manning، نويسنده , , H. Charles and Bai، نويسنده , , Mingfeng and Anderson، نويسنده , , Bernard M. and Lisiak، نويسنده , , Rafal and Samuelson، نويسنده , , Lynn E. and Bornhop، نويسنده , , Darryl J.، نويسنده ,
Abstract :
Phosphonic acid appended tetraazacyclododecane (cyclen)-based macrocycles are attractive metal-ion chelators for diagnostic imaging and therapeutic delivery. Here, we report a novel P-protected methodology that facilitates the rapid synthesis and purification of targeted phosphonic acid bearing macrocycles. Purification of these intermediates is facile, and deprotection using neat TFA is rapid, yet mild enough to preserve the integrity of delicate peptides and/or targeting moieties.