High-activity Pt complex as well as preparation method and application thereof
A complex and highly active technology, which can be applied in pharmaceutical formulations, organic active ingredients, platinum group organic compounds, etc., can solve the problems of discounting therapeutic efficacy and limiting clinical use, and achieve simple and easy preparation methods and overcome cisplatin resistance Sexuality, the effect of great application prospects
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[0024] Preparation of compound a2:
[0025] 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 a2 as a yellow solid with a yield of 87%.
Embodiment 1
[0027] A kind of highly active Pt (IV) complex, its preparation method comprises the steps:
[0028]
[0029] Add 0.42 g compound a2 (1.26 mmol) and 0.80 g compound b (3.80 mmol) to 10 ml DMF solution, then add 1.22 g TBTU (3.80 mmol) and 0.38 g (3.80 mmol) triethylamine, and react at 25°C for 72 h, after the reaction, the solvent was evaporated under reduced pressure, 20 mL of methanol was added, solids were precipitated, filtered, and the filter cake was rinsed with methanol, evaporated to dryness under reduced pressure to obtain a brown solid, complex 1; 1 H NMR, 13 C NMR and MS characterize the brown solid product obtained, and the obtained data are as follows:
[0030] 1 H-NMR (400 MHz, DMSO-d6): δ (ppm) 7.85 (d, J = 1.7 Hz, 2H), 7.78 (d, J = 8.4 Hz, 2H), 7.39 (dd, J = 8.3, 1.8 Hz , 2H), 6.79 (br, 6H), 2.48 (s, 6H).
[0031] 13 C-NMR (400 MHz, DMSO-d6): δ (ppm) 166.86, 153.61, 142.53, 132.10, 128.38, 124.13, 122.98, 122.73, 112.48, 10.00
[0032] ESI-MS(negative ...
Embodiment 2
[0034] A kind of highly active Pt (IV) complex, its preparation method comprises the steps:
[0035]
[0036] Add 0.10 g compound a2 (0.30 mmol) and 0.19 g compound c (0.90 mmol) to 10 ml DMF solution, then add 0.29 g TBTU (0.90 mmol) and 0.09 g (0.90 mmol) triethylamine, and react at 25°C for 72 h, after the reaction, the solvent was evaporated under reduced pressure, 20 mL of methanol was added, solids were precipitated, filtered, and the filter cake was rinsed with methanol, evaporated to dryness under reduced pressure to obtain a brown solid, complex 1; 1 H NMR, 13 C NMR and MS characterize the brown solid product obtained, and the obtained data are as follows:
[0037] 1 H-NMR (400 MHz, DMSO-d6): δ (ppm) δ (ppm) 7.63 (s, 2H), 7.49 (d, J =8.7 Hz, 2H), 7.43 (d, J = 8.9 Hz, 2H) , 6.79 (br, 6H), 2.60 (s, 6H).
[0038] 13 C-NMR (400 MHz, DMSO-d6): δ (ppm) 161.56, 153.72, 141.35, 133.20, 128.72, 127.37, 124.60, 120.58, 112.93, 9.53
[0039] ESI-MS (positive mode, m / z) ...
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