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ASGPR-targeted positive electron developer as well as preparation method and application thereof

A positron imaging agent and targeting technology, which is applied in the preparation of sugar derivatives, organic chemical methods, chemical instruments and methods, etc., can solve the problems of multimer synthesis difficulties, false positives, and affecting the diagnosis of abdominal diseases, and achieve Good imaging effect and strong affinity

Active Publication Date: 2019-02-22
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, most of the ASGPR labeling technologies have the following disadvantages: 1) The synthesis of Gal / GalNAc analog polymers is difficult and costly; 2) The heterogeneity and heterogeneity of tumor surface receptors lead to the targeting and affinity of probes Insufficient; 3) The ratio of tumor target / non-target is not high; 4) The obvious uptake of non-tumor lesions (such as tuberculosis, granuloma, inflammatory pseudotumor, etc.) leads to false positives; 5) High uptake of kidney and liver will affect Diagnosis of Abdominal Disorders

Method used

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  • ASGPR-targeted positive electron developer as well as preparation method and application thereof
  • ASGPR-targeted positive electron developer as well as preparation method and application thereof
  • ASGPR-targeted positive electron developer as well as preparation method and application thereof

Examples

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preparation example Construction

[0035] The preparation method of the above-mentioned positron imaging agent targeting ASGPR comprises the following steps:

[0036] 1) Disperse 4-pentyn-1-ol in a solvent, then add triethylamine, 4-dimethylaminopyridine and p-toluenesulfonyl chloride, fully react, extract the reaction solution, and then remove water from the extract , vacuum distillation and column chromatography to obtain

[0037] 2) Will dispersed in a solvent, and then added 18 F ions, fully reacted, get

[0038] 3) Will Disperse in the solvent, then add 4A molecular sieve, mix evenly, then add trimethylsilane azide and tin tetrachloride, fully react, remove 4A molecular sieve by suction filtration, then dewater the filtrate, vacuum distillation and column layer analyzed and separated to obtain

[0039] 4) Will Disperse in a solvent, then add sodium methoxide, fully react, adjust the pH value of the reaction solution to 6-7, filter and dry to obtain

[0040] 5) Will dispersed in a solven...

Embodiment 1

[0057] A preparation method of a positron imaging agent targeting ASGPR, comprising the following steps:

[0058] 1) Disperse 4-pentyn-1-ol (2.52g, 30mmol) in 80mL of dichloromethane, then add triethylamine (10.12g, 100mmol), 4-dimethylaminopyridine (0.16g, 1.32mmol) and p-toluenesulfonyl chloride (6.86g, 36mmol), reacted at room temperature for 14h, then extracted with ethyl acetate, and then subjected to anhydrous sodium sulfate dehydration, vacuum distillation and column chromatography to separate the extract to obtain a light yellow liquid Yield 39%; 1 H NMR (600MHz, CDCl 3 )δ7.80(d, J=8.3Hz, 2H), 7.35(d, J=8.1Hz, 2H), 4.15(t, J=6.1Hz, 2H), 2.44(d, J=13.4Hz, 3H) ,2.26(dt,J=6.9,2.6Hz,2H),1.86(m,2H),1.23(m,1H);

[0059] 2) Will (35.7mg, 0.15mmol) was dispersed in 1mL acetonitrile, then added 18 F ions (100mCi), reacted at 85°C for 10min to obtain Yield 40%;

[0060] 3) Will (3.9g, 10mmol) was dispersed in 20mL of ultra-dry dichloromethane, then an appropriate amo...

Embodiment 2

[0069] A preparation method of a positron imaging agent targeting ASGPR, comprising the following steps:

[0070] 1) Disperse 4-pentyn-1-ol (2.52g, 30mmol) in 80mL of dichloromethane, then add triethylamine (10.12g, 100mmol), 4-dimethylaminopyridine (0.16g, 1.32mmol) and p-toluenesulfonyl chloride (6.86g, 36mmol), reacted at room temperature for 12h, then extracted with ethyl acetate, and then subjected to anhydrous sodium sulfate dehydration, vacuum distillation and column chromatography to separate the extract to obtain a light yellow liquid Yield 36%;

[0071] 2) Will (35.7mg, 0.15mmol) was dispersed in 1mL acetonitrile, then added 18 F ions (100mCi), reacted at 85°C for 15min to obtain Yield 38%;

[0072] 3) Will (3.9g, 10mmol) was dispersed in 20mL of ultra-dry dichloromethane, then an appropriate amount of freshly evaporated 4A molecular sieves was added, stirred for 20min, then trimethylsilyl azide (1.38g, 12mmol) and tin tetrachloride ( 4.168g, 16mmol), stirr...

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Abstract

The invention discloses an ASGPR-targeted positive electron developer as well as a preparation method and application thereof. The positive electron developer is capable of specifically targeting tumors such as HepG2, A549, MDA-MB-231, MCF-7 and the like with high ASGPR expressivity, has strong affinity with ASGPR expressed in tumor cells, has a good development effect and is taken as a potentialreceptor developer, and a novel way is provided for the PET / CT clinical diagnosis.

Description

technical field [0001] The invention relates to a positron imaging agent targeting ASGPR, a preparation method and application thereof. Background technique [0002] PET tumor receptor imaging (Tumor Receptor Imaging) is the principle of combining the corresponding ligands labeled with positron radionuclides with specific receptors that are highly expressed in tumors and have high affinity with target tissues, and can display the spatial distribution and density of tumor receptors. Imaging technology with affinity. PET tumor receptor imaging has high affinity, strong specificity, strong penetrating ability, radiolabeled ligand reaches the target and clears the blood quickly, and can obtain high-contrast images of tumors and normal tissues in a short period of time. It has advantages such as the occurrence of human immune response, and it is also non-invasive, and it can conduct research at the cell and molecular level in a living state, which is one of the important develop...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/056C07H1/00A61K51/04A61K101/02
CPCA61K51/0491A61K51/0497C07H1/00C07H19/056C07B2200/05
Inventor 孙朋辉胡孔珍黄顺韩彦江王猛王全师吴湖炳谭建儿王丽娟
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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