Low-toxicity Pt complex and preparation method and application thereof
A complex and low-toxicity technology, applied in platinum group organic compounds, chemical instruments and methods, platinum-based organic compounds, etc., can solve the problems of poor tumor targeting and strong side effects
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[0037] Preparation of compound c1:
[0038] Add 3.00 g of cisplatin (10.00 mmol) into 180 mL of hydrogen peroxide (30%-35%) solution, avoid light, heat up to 75°C for 7 h, cool down to room temperature, refrigerate overnight, filter, The filter cake was washed with a small amount of cold water, the solid was collected and evaporated to dryness under reduced pressure to obtain 2.90 g of compound c1 as a yellow solid with a yield of 87%.
Embodiment 1
[0040] A kind of low toxicity Pt (IV) complex, its preparation method comprises the steps:
[0041]
[0042] Add 1.00 g of compound a1 (3.90 mmol) and 0.37 g of chloroacetic acid (4.29 mmol) into 10 ml of ethanol solution, add 0.31 g of sodium hydroxide aqueous solution (10 ml) dropwise under ice-cooling, after the addition is complete, heat up to 65°C and react overnight , after the TLC detection reaction is complete, add ethyl acetate to wash twice, adjust the aqueous phase to pH 4-5 with aqueous citric acid, extract twice with ethyl acetate, combine the organic phases, dry the organic phases with anhydrous sodium sulfate, and filter , and evaporated to dryness under reduced pressure to obtain 1.0 g of white solid compound a with a yield of 81%;
[0043] 1 H-NMR (400 MHz, CDCl3): δ (ppm) 7.47 (d, J = 8.5 Hz, 2H), 7.03 (d, J = 16.2 Hz, 1H), 6.97-6.92 (m, 3H), 6.65 (d , J = 2.2 Hz, 2H), 6.36 (d, J = 2.4Hz, 1H), 4.70 (s, 2H), 3.83 (s, 6H).
[0044](2) 0.80 g of compound a...
Embodiment 2
[0050] A kind of low toxicity Pt (IV) complex, its preparation method comprises the steps:
[0051] 283 mg of compound c1 (0.85 mmol) was mixed with 10 mL of dry DMF, and 800 mg of compound a (2.55 mmol), 257 mg of triethylamine (2.55 mmol) and 817 mg of TBTU (2.55 mmol) were added in sequence, and the addition was completed at room temperature. Stirred for 48 h, after the reaction was over, the reaction solvent was concentrated to about 5 mL, methanol was added for crystallization, filtered, the filter cake was washed twice with methanol, and dried under reduced pressure to obtain a pale yellow solid, complex 2; 1 H NMR, 13 The resulting pale yellow solid product was characterized by C NMR and MS, and the data obtained are as follows:
[0052] 1 H-NMR (400 MHz, DMSO-d6): δ (ppm) 7.51 (d, J = 8.8 Hz, 2H ), 7.22 (d, J = 16.3, 1H), 7.03 (d, J = 16.4, 1H), 6.95(d, J = 8.7 Hz, 2H), 6.75(d, J= 2.2 Hz, 2H), 6.62(br, 6H), 6.36(s, 1H), 4.66(s, 2H) , 3.78(s, 6H) ).
[0053] 13 ...
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