A small molecule organic nanometer tumor photothermal therapy reagent and its preparation method
A photothermal therapy and small molecule technology, applied in organic chemistry, antineoplastic drugs, medical preparations containing active ingredients, etc., can solve the problems of no specific targeting, poor biocompatibility, poor water solubility, etc. Excellent targeting, reduced toxicity and side effects, clear structure effect
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Embodiment 1
[0031]3,6-bis(5-(4-(4-(dimethylamino)benzoyl)benzene-2-thienyl)-2,5-bis(1-bromo-hexane)pyrrolo[3,4 -c] Synthesis of pyrrole-1,4-dione (ie DPP-R1):
[0032] Under nitrogen protection, 3,6-bis(2-thienyl)-2,5-bis(1-bromo-hexane)pyrrolo[3,4-c]pyrrole-1,4-dione (0.780 g, 1 mmol), p-dimethylaminobenzophenone (0.562 g, 2.5 mmol), palladium acetate (0.006 g, 0.025 mmol), trimethylacetic acid (0.015 g, 0.15 mmol), anhydrous potassium carbonate (0.345 g, 2.5 mmol) was added to 25 ml of anhydrous N, N-dimethylacetamide, stirred at 100 ° C for 4 hours, washed with water, extracted with DCM to remove DMF to obtain a crude product, and the crude product was separated by silica gel chromatography DPP-R1 (0.612 g, 60% yield) was obtained.
[0033] Add 150 microliters of 4 mg / ml DPP-R1 tetrahydrofuran solution slowly (dropping speed: 25-30 drops / min) into 10 ml of water with rapid stirring (1000 rpm), stir for 5 minutes, and fill with nitrogen The tetrahydrofuran in the solution was blown a...
Embodiment 2
[0043] 3,6-bis(5-(4-(diphenylamine)benzene-2-thienyl)-2,5-bis(1-bromo-hexane)pyrrolo[3,4-c]pyrrole-1,4 - Synthesis of diketone (i.e. DPP-R2):
[0044] Under nitrogen protection, 3,6-bis(2-thienyl)-2,5-bis(1-bromo-hexane)pyrrolo[3,4-c]pyrrole-1,4-dione (0.780 g, 1 mmol), p-triphenylamine (0.615 g, 2.5 mmol), palladium acetate (0.006 g, 0.025 mmol), trimethylacetic acid (0.015 g, 0.15 mmol), anhydrous potassium carbonate (0.345 g, 2.5 millimol) was added to 25 milliliters of anhydrous N, N-dimethylacetamide, stirred at 110°C for 10 hours, washed with water, extracted with DCM to remove DMF to obtain a crude product, and the crude product was separated with a silica gel column to obtain DPP-R2 ( 0.820 g, yield 74%).
[0045] 150 μL of 4 mg / mL –1 DPP-R2 tetrahydrofuran solution, slowly dropwise (dropping speed is 15-20 drops / min) into 10ml water of rapid stirring (2000 rpm), after stirring for 5 minutes, blow off the tetrahydrofuran in the solution with nitrogen gas, and then ...
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