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Radioactive iodine-17- allylamino-17-demethoxygeldanamycin and its preparation method

A technology of methoxygeldanamycin and radioactive iodine is applied in the fields of oncology, nuclear medicine, and pharmaceutical preparation, which can solve the problems such as research in the ascendant, and achieve the advantages of small polarity, simple preparation process and good medicinal prospects. Effect

Inactive Publication Date: 2010-12-08
SOUTHEAST UNIV
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  • Application Information

AI Technical Summary

Problems solved by technology

[0005] With the in-depth research on the pathogenesis of tumors at the molecular level, researchers have found that heat shock protein 90 (Heat-Shock Proteins 90, HSP90), which acts as a molecular chaperone in vivo, plays an important role in the development of tumors. Research on inhibitors of the target is in the ascendant

Method used

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  • Radioactive iodine-17- allylamino-17-demethoxygeldanamycin and its preparation method
  • Radioactive iodine-17- allylamino-17-demethoxygeldanamycin and its preparation method

Examples

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Embodiment

[0037] (1): * Preparation of I-17-propylamino-17-desmethoxygeldanamycin

[0038]

[0039] 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 0.01 mol / L sodium metabisulfite to terminate the reaction. Adjust the pH to 7 with ammonia water.

[0040] 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.

[0041] 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, so...

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Abstract

The invention discloses a making method of radioactive iodine-17-allylamine-17-normethoxy geldanamycin in the nuclear medical, tumour and medical agent technical domain, which is characterized by the following: marking the product of 17-allylamine-17-normethoxy geldanamycin through iodine for HSP90; modifying the structure of 17-allylamine-17-normethoxy geldanamycin; guiding radioactive nuclear iodine on the end of double-bond; providing the medical acceptable drug or drug composition to treat tumor or cancer.

Description

technical field [0001] The invention relates to a tumor treatment reagent radioactive iodine ( * I)-17-propylamino-17-desmethoxygeldanamycin, tumor diagnostic agent (single photon emission computed tomography / SPECT, positron emission computed tomography / PET) and medicines thereof or Preparation method and application of pharmaceutical composition. It involves the technical fields of nuclear medicine, oncology, and pharmaceutical preparations. Background technique [0002] Malignant tumors are diseases that seriously threaten human survival and health, and early diagnosis is difficult. In recent years, the morbidity and mortality of tumors have been increasing year by year. The loss of surgical opportunities and recurrence and metastasis after surgery are the main reasons that make tumors difficult to control and accelerate the death of patients. At present, the treatment of tumors mainly relies on comprehensive measures such as surgery, chemotherapy, radiotherapy and biol...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/04A61K101/02C07D225/06C07B59/00
Inventor 刘璐杨敏姜新宇陈道桢罗世能孙晋高文黄鹰
Owner SOUTHEAST UNIV
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