Organic nano-assembly for biological imaging in second window of near-infrared region, as well as preparation method and application of organic nano-assembly
A nano-assembly, organic technology, applied in the preparations for in vivo experiments, nanotechnology, nanotechnology, etc., can solve the problem of lack of targeting and activatable characteristics, limited time window, and inability to achieve specific lighting And other issues
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Embodiment 1
[0057] Preparation of NIRlyso-NP-PEG1000 nanometer assembly, the monomer structure of the assembly is as follows:
[0058]
[0059] Concrete synthetic route is as follows:
[0060]
[0061] Concrete synthetic steps are as follows:
[0062] (1) Synthesis of intermediate 1-1
[0063] Dissolve p-bromo-substituted thiophenol (compound 1-1) and ethyl substituted phenylacetoacetate (compound 1-2) in polyphosphoric acid, react at 90-100°C for 1-3 hours; add crushed The reaction was quenched with ice, extracted with dichloromethane, and the organic phase was concentrated and separated by column chromatography to obtain intermediate 1-1; wherein the molar ratio of compound 1-1, compound 1-2 and polyphosphoric acid was 1:(1.~ 1.3): (10~15);
[0064] (2) Synthesis of intermediate 1-2
[0065] Under the protection of nitrogen, the intermediate 1-1, tert-butoxycarbonylpiperazine, Buchwald catalyst and inorganic base were mixed in a dry solvent, and reacted at 80-110°C for 3-12 ho...
Embodiment 2
[0079] Preparation of NIRlyso-NP-PEG2000-RGD nano-assembly, the monomer structure of the assembly is as follows:
[0080]
[0081] Concrete synthetic route is as follows:
[0082]
[0083] Concrete synthetic steps are as follows:
[0084] (1) Synthesis of intermediate 2-1
[0085] Intermediate-6 and azide-polyethylene glycol-succinimide chain (compound 6-1) were dissolved in dichloromethane, and cuprous iodide, azidodiisopropylethylamine and acetic acid were added successively as Catalyst, stirred at room temperature in the dark for 8-24 hours. The reaction solution was centrifuged at high speed to remove the precipitate, the organic phase was concentrated and separated by reverse column chromatography to obtain intermediate 2-1; wherein intermediate 1-6, compound 2-1, cuprous iodide, nitrogen nitrogen diisopropylethylamine and The feeding molar ratio of acetic acid is 1:(1~1.5):(0.01~0.1):(0.01~0.1):(0.01~0.1).
[0086] (2) Preparation of product 2 from intermediate...
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