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Diagnosis and treatment integrated compound as well as preparation method and application thereof

One compound, one technology, applied in the field of medicine, can solve problems such as undeveloped cancer treatments

Pending Publication Date: 2020-09-25
JIANGSU FOOD & PHARMA SCI COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Unfortunately, effective and clinically effective cancer treatments have not yet been developed, creating an urgent need for novel potent and specific anticancer drugs

Method used

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  • Diagnosis and treatment integrated compound as well as preparation method and application thereof
  • Diagnosis and treatment integrated compound as well as preparation method and application thereof
  • Diagnosis and treatment integrated compound as well as preparation method and application thereof

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preparation example Construction

[0043] In the second aspect, the embodiment of the present invention also proposes a method for preparing the integrated compound of diagnosis and treatment as described above, including the following steps: synthesizing Boc-2,3,5-triiodobenzoic acid: combining 2,3,5-triiodobenzene Formic acid was dissolved in t-BuOH, then DPPA and TEA were added, and the mixture was stirred at 85-95 °C for 1.5-2.5 h under a nitrogen atmosphere, then the mixture was desolvated under reduced pressure, the residue was dissolved in DCM, washed with saturated NaHCO 3 The organic phase was obtained by washing, and then the organic phase was washed with anhydrous Na 2 SO 4 After drying, the organic phase was concentrated, and the residue was purified by silica gel column chromatography, eluting with PE / EA, to obtain Boc-2,3,5-triiodobenzoic acid; to synthesize 2,3,5-triiodoaniline: Boc -2,3,5-Triiodobenzoic acid dissolved in CH 2 Cl 2 In solution, at -5-5°C to CH of Boc-2,3,5-triiodobenzoic acid ...

Embodiment 1

[0052] The preparation method of the integrated compound of diagnosis and treatment comprises the following steps: synthesizing Boc-2,3,5-triiodobenzoic acid: dissolving 2,3,5-triiodobenzoic acid in t-BuOH. Then DPPA and TEA were added, and the mixture was stirred at 85 °C under nitrogen atmosphere for 1.5 h, then the mixture was desolvated under reduced pressure, the residue was dissolved in DCM, washed with saturated NaHCO 3 The organic phase was obtained by washing, and then the organic phase was washed with anhydrous Na 2 SO 4 After drying, the organic phase was concentrated, and the residue was purified by silica gel column chromatography, eluting with PE / EA (V:V=10:1), to obtain Boc-2,3,5-triiodobenzoic acid;

[0053] Synthesis of 2,3,5-triiodoaniline: Dissolving Boc-2,3,5-triiodobenzoic acid in CH 2 Cl 2 In solution, at -5°C to CH of Boc-2,3,5-triiodobenzoic acid 2 Cl 2 TFA was added to the solution, and after consumption of the starting material, the mixture was e...

Embodiment 2

[0057] The preparation method of the integrated compound of diagnosis and treatment comprises the following steps: synthesizing Boc-2,3,5-triiodobenzoic acid: dissolving 2,3,5-triiodobenzoic acid in t-BuOH. Then DPPA and TEA were added, and the mixture was stirred at 95°C under nitrogen atmosphere for 2.5 hours, then the mixture was desolvated under reduced pressure, the residue was dissolved in DCM, washed with saturated NaHCO 3 The organic phase was obtained by washing, and then the organic phase was washed with anhydrous Na 2 SO 4 After drying, the organic phase was concentrated, and the residue was purified by silica gel column chromatography, eluting with PE / EA (V:V=10:1), to obtain Boc-2,3,5-triiodobenzoic acid;

[0058] Synthesis of 2,3,5-triiodoaniline: Dissolving Boc-2,3,5-triiodobenzoic acid in CH 2 Cl 2 In solution, at 5°C to CH of Boc-2,3,5-triiodobenzoic acid 2 Cl 2 TFA was added to the solution, and after consumption of the starting material, the mixture was...

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Abstract

The invention relates to the technical field of medicines, and particularly discloses a diagnosis and treatment integrated compound as well as a preparation method and application thereof. The diagnosis and treatment integrated compound is a vorinostat derivative, wherein at least one iodine atom is introduced to a benzene ring of vorinostat; the compound not only has anti-tumor activity, but alsohas a diagnostic imaging function. The preparation method of the diagnosis and treatment integrated compound comprises the following steps that Boc-2,3,5-triiodobenzoic acid is synthesized, 2,3,5-triiodobenzidine is synthesized, and the 8-oxo-8-((2,3,5-triiodobenzyl) amino) methyl caprylate is synthesized. The preparation methos is simple; the invention also discloses application of a diagnosis and treatment integrated compound, wherein the compound is applied to antitumor medicines so as to be used for anti-tumor treatment and diagnosis imaging functions of tumor patients.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular, to a compound for diagnosis and treatment, a preparation method and an application thereof. Background technique [0002] Cancer is one of the leading causes of death worldwide, killing nearly 8 million people every year and causing major socioeconomic harm to the entire human race. Unfortunately, effective and clinically effective cancer treatments have not yet been developed, creating an urgent need for novel potent and specific anticancer drugs. [0003] Histone acetyltransferases (HATs) and histone deacetylases (HDACs) have recently become important targets for cancer therapy. Indeed, several HDAC inhibitors have been used to treat T-cell lymphoma, including SAHA (sulfenyl anilide hydroxamic acid, vorinostat) and Belinostat. Panobinostat was recently approved for the treatment of multiple myeloma. [0004] At the same time, early diagnosis of cancer is also very important t...

Claims

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Application Information

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IPC IPC(8): C07C259/06A61K49/04A61P35/00
CPCC07C259/06A61K49/0438A61P35/00
Inventor 金乐代浩男陆睿王艳翠
Owner JIANGSU FOOD & PHARMA SCI COLLEGE
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