Radioactive iodine-17- allylamino-17-demethoxygeldanamycin and its preparation method
A technology based on methoxygeldanamycin and allylamine, which is applied in the fields of oncology, pharmaceutical preparations, and nuclear medicine. It can solve problems such as research in the ascendant, achieve low polarity, reduce toxic and side effects, enhance polarity and targeted effect
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[0040] (1): * Preparation of I-17-propenylamino-17-desmethoxygeldanamycin
[0041]
[0042] A: Dissolve 20 μg of 17-propenylamino-17-desmethoxygeldanamycin in 100 μL of ethanol, add 20 μL of 4mol / L hydrochloric acid solution, add 20 μL of 7% hydrogen peroxide, 37~370MBq (1~10mCi)Na * I. Vortex for 1 min to mix evenly, and place at 40°C for 15 min; add 0.01mol / L sodium metabisulfite to terminate the reaction. Adjust the pH to 7 with ammonia water.
[0043] B: Add 2 mL of water to A, extract with ethyl acetate (3 mL x 3 times), collect the organic phase, blow dry with nitrogen, and obtain the product.
[0044] Na * Iodine in I ( * I) is the nuclide iodine 123 I. 124 I. 125 I. 127 I. 131 A kind of in I; Oxidant is hydrogen peroxide, a kind of in peracetic acid; Acidic condition is a kind of in hydrochloric acid, acetic acid, sulfuric acid; Reducing agent is a kind of in sodium metabisulfite, sodium thiosulfate; pH adjuster is One of sodium hydroxide, ammonia water, s...
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