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Novel F-triazole ring-polyethyleneglycol-2-nitroimidazole compound and preparation method thereof

A technology of polyethylene glycol and nitroimidazole, applied in the field of nitroimidazole compounds and preparation thereof, can solve problems such as research results reporting

Inactive Publication Date: 2014-07-09
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, no further research results have been reported

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  • Novel F-triazole ring-polyethyleneglycol-2-nitroimidazole compound and preparation method thereof
  • Novel F-triazole ring-polyethyleneglycol-2-nitroimidazole compound and preparation method thereof
  • Novel F-triazole ring-polyethyleneglycol-2-nitroimidazole compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1- Embodiment 4

[0059] Embodiment 1-embodiment 4 ( 19 Synthesis of F)

Embodiment 1

[0061] 1. Synthesis of Intermediate Alkynes

[0062] Synthesis of PETY-1 (m=1)

[0063] (1) The structure of compound PETY-1

[0064]

[0065] (2) Synthesis method

[0066] a. Synthesis of PEGY-1

[0067] Add propyne bromide (5.34g, 45mmol) and ethylene glycol (5.57g, 20mmol) into a 25mL three-neck flask under the protection of argon, slowly add NaOH into the reaction flask under stirring in an ice bath, and keep the ice-water bath for 15min. Then heated to reflux at 40°C for 3h. After the reaction was completed, it was filtered, and the solid was washed with ethyl acetate. The filtrate was washed with a small amount of water until neutral. Na for organic phase 2 SO 4 Dry, filter, remove the solvent under reduced pressure, and perform column chromatography, the solvent ratio is ethyl acetate:n-hexane=1:3. The product fractions were collected, and the solvent was removed under reduced pressure to obtain 1.50 g of a yellow oil, with a yield of 34.2%.

[0068] 1 HNMR...

Embodiment 2

[0096] The synthesis of the intermediate alkyne is the same as in Example 1.

[0097] Synthesis of Compound NIA2-TAF (n=1, m=1)

[0098] (1) The structure of the compound NIA2-TAF

[0099]

[0100] (2) Synthesis method

[0101] a. Synthesis of Compound PETA-2

[0102]Ethylene glycol (4.24 g, 40 mmol, 3.9 mL) was dissolved in 30 mL of dichloromethane. Under the condition of ice-water bath, p-toluenesulfonyl chloride (18.30g, 96mmol) was added to the above solution, and then sodium hydroxide (6.40g, 160mmol) was added slowly, and the reaction was stirred at 0-5°C for 2-3h in ice-water bath. After the reaction was completed, 50 mL of dichloromethane and 30 mL of ice water were added, shaken, and separated into layers. The organic phase was washed successively with hydrochloric acid solution, saturated sodium bicarbonate solution, and ice water until neutral, Na 2 SO 4 After drying, the solvent was removed under reduced pressure to obtain a crude product. The crude produ...

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PUM

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Abstract

The invention relates to a novel F-triazole ring-PEG-2-nitroimidazole compound and a preparation method thereof, and the structural general formula of the compound is shown in the description, wherein n=0, 1, 2, 3, 4; and m=1, 2, 3. A triazole ring, a PEG group, 2-nitroimidazole and a <18 / 19>F nuclide are connected by using nitroimidazole as a targeting group by a click method, and are designed to synthesize a series of novel F-triazole ring-polyethyleneglycol-2-nitroimidazole derivatives, and the nitroimidazole derivative is used as a novel compound capable of improving the metabolic property of medicaments and is used for PET anaerobic visualization studies.

Description

technical field [0001] The invention relates to a nitroimidazole compound and a preparation method thereof, in particular to a novel F-triazole ring-polyethylene glycol-2-nitroimidazole compound and a preparation method thereof. Background technique [0002] With the rapid increase in the number of PET imaging instruments and the increasing demand for positron drugs, the development of PET drugs is developing rapidly. 18 F is the most important nuclide of choice in PET drugs, and it plays an extremely important role in the development and application of positron drugs, and has become a hot spot in the current radiopharmaceutical research. [0003] "Click" chemistry, often translated as "click" chemistry or "link" chemistry, was proposed in 2001 by Nobel Prize winner Sharpless et al. A synthetic technique that has brought major innovations to traditional organic synthetic chemistry has been widely used in the preparation of various fields such as chemistry, medicine, and mat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D403/06C07D403/12A61K51/04A61K101/02
Inventor 朱霖杜风华刘亚静
Owner BEIJING NORMAL UNIVERSITY
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