<p>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 (PCl<sub>3</sub> and H<sub>3</sub>PO<sub>3</sub>) followed by hydrolysis. TyrBP was characterized using IR, NMR, and mass spectroscopy, and underwent a <sup>99m</sup>Tc-radiolabeling study to produce a potential bone imaging agent using sodium borohydride as a reducing agent for <sup>99m</sup>Tc eluted from the <sup>99</sup>Mo/<sup>99m</sup>Tc generator. Optimization of the radiolabeling conditions was performed to achieve a high radiochemical yield.</p>

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

  • Walid Hamouda,
  • Mohamed Abdel-Motaleb,
  • Mahmoud El-Tawoosy,
  • Mahmoud Sanad,
  • Sameh Rizk,
  • Maher El-Hashash

摘要

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.