Technetium-99m marked 6-hydrazino pyridine-3-formamido novel lactose albumin complexes, preparation and use thereof
A technology of hydrazinopyridine and -99m, which is applied in the field of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems of slow liver clearing and low non-target organ uptake, and achieve the effect of high ratio, simple preparation and low cost of use
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[0036] The present invention is described in detail below through examples, a technetium-99m-labeled 6-hydrazinopyridine-3-carboxamide-based neolactoalbumin complex:
[0037] (1) Preparation of ligand HYNIC-NGA:
[0038] HCl gas was passed through dioxane at an appropriate rate for 10 minutes to obtain a solution of HCl in dioxane. Dissolve 100mg of succinimide-6-tert-butoxycarbonylhydrazinopyridine-3-carboxylic acid in 2mL of dioxane, add 2mL of HCl / dioxane after all dissolved, and stir the reaction at room temperature mixture. After 5 minutes, the solution became cloudy and a precipitate formed. Stirring was continued in the dark for 4 hours. The turbid reaction mixture was filtered, and the solid was washed repeatedly with ether to obtain 55 mg of a white solid. Yield 67%.
[0039] Weigh 100 mg of NGA and dissolve it in 5 mL of 0.2 mol / L pH8.6 boric acid buffer at a concentration of about 20 mg / mL. Succinimid-6-ylhydrazinopyridine-3-carboxylic acid (6.5 mg dissolved i...
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