Radiotracer precursor for imaging of hypoxic tissue, radiotracer, and method for preparing the same

摘要

A radiotracer precursor for imaging of hypoxic tissues, a radiotracer and a method for preparing the same are revealed. The radiotracer precursor, DANI, includes a nitroimidazole functional group with a feature of retention in hypoxic tissues and a bifunctional ligand able to complex with radioisotopes. Thus DANI can be used to produce radiotracers stayed in hypoxic tissues and the radiotracers are applied to medical imaging of malignant tumor with hypoxic layer.

主权项

1. A method for preparing a radiotracer precursor comprising the steps of:
using 6-amino-1-hexanol and tert-butyl carbonate to carry out amino group protection and get tert-butyl 6-hydroxycarbamate; using tert-butyl 6-hydroxycarbamate and P-toluenesulfonyl chloride to perform a substitution reaction in pyridine solution and produce tert-butyl 6-toluenesulfonyl hexylcarbamate; taking tert-butyl 6-toluenesulfonyl hexylcarbamate and 2-nitroimidazole to perform substitution reaction in dimethylformamide (DMF) solution and get tert-butyl 6-(2-nitroimidazole)hexylcarbamate; and hydrogenizing tert-butyl 6-(2-nitroimidazole) -hexylcarbamate to get 6-(2-nitroimidazole)hexylamine and 6-(2-nitroimidazole)hexylamine further reacting with L-3,6-diaza-4,7-dioxo-8-[(triphenylmethyl) -thio]-2-[((triphenylmethyl)thio)methyl]octanoic acid to carry out amidation and get (6-(2-nitroimidazde)hexyl-L-3,6-diaza-4,7-dioxo -8[(triphenylmethyl)thio]-2-[((triphenylmethyl)thio)m ethyl]octanamide (DANI).