Convenient Route for Synthesis of Bifunctional Chelating Agent:l-(p-Aminobenzyl)ethylenediaminetetramethylphosphonic acid-Folate Conjugate (Am-Bz-EDTMP-Folate)

摘要

The present work describes a convenient and efficient approach for the synthesis of bifunctional chelating agent,1-(p-aminobenzyl)ethylenediaminetetramethylphosphonic acid (Am-Bz-EDTMP).The key steps involved are functionalization of L-phenylalanine to give ethylenediaminetetraacetic acid derivative and its conversion to phosphonic acid followed by the reaction with NHS-folate to give l-(p-aminobenzyl)-EDTMP-folate conjugate to be used for targeted radio imaging and therapy.Radiolabeling with ~(III)In and ~(153)Sm of Folate-Bz-EDTMP conjugate showed very high stability under physiological conditions.