99mTc-radiolabeling study of 2-amino-3-(4-hydroxyphenyl)-1-hydroxypropyl-1,1-bisphosphonic acid as a potential bone imaging agent

Abstract 2-Amino-3-(4-hydroxyphenyl)-1-hydroxypropyl-1,1-bisphosphonic acid (TyrBP), a nitrogenated bisphosphonate (NBP), has been synthesized in a one-pot two-step process involving the phosphonation of L-tyrosine with phosphorus reagents (PCl3 and H3PO3) followed by hydrolysis. TyrBP was characterized using IR, NMR, and mass spectroscopy, and underwent a 99mTc-radiolabeling study to produce a potential bone imaging agent using sodium borohydride as a reducing agent for 99mTc eluted from the 99Mo/99mTc generator. Optimization of the radiolabeling conditions was performed to achieve a high radiochemical yield.