A kind of phenylthiazole derivative and its preparation method and application
A technology of phenylthiazole and derivatives is applied in the application field of preparing gastric cancer treatment-related drugs, and can solve the problems of malignant cell proliferation, lipid and protein synthesis disorder and the like
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Embodiment 1
[0045] Synthesis and characterization of compound 1a:
[0046]
[0047] Take compound (2a) 1.1g (5.18mmol), compound (3a) 0.84g (5.18mmol), HOBT 2.09g (15.5mmol), HBTU 5.87g (15.5mmol) into a 100ml round bottom flask, add redistilled Add 8.1ml (46.6mmol) of DIPEA to 40ml of DMF, and stir at room temperature for 4h. After the reaction, the reaction solution was diluted with 200ml of ethyl acetate, washed with water (50ml×5) to remove DMF, and the organic phase was washed with anhydrous Na 2 SO 4 It was dried for 1 h, filtered, and the filtrate was spin-dried and passed through the column to obtain 1.46 g of white solid (4a), with a yield of 78%.
[0048] Take 0.9g (2.57mmol) of compound (4a), add 1.06g (7.11mmol) of potassium carbonate into a 50ml round-bottomed flask, add 25ml of redistilled DMF, slowly add 0.6ml (7.11mmol) of iodoethanol dropwise, and stir the reaction at 50°C 12h. After the reaction, the reaction solution was diluted with 100ml of ethyl acetate, washe...
Embodiment 2
[0053] Synthesis and characterization of compound 1b:
[0054]
[0055] Take compound (2b) 1.73g (6mmol), compound (3b) 1.33g (6mmol), HOBT 2.43g (18mmol), HBTU 6.83g (18mmol) into a 100ml round bottom flask, add redistilled DMF 40ml under nitrogen protection, Add DIPEA8.92ml (54mmol), and stir at room temperature for 4h. After the reaction, the reaction solution was diluted with 200ml of ethyl acetate, washed with water (50ml×5) to remove DMF, and the organic phase was washed with anhydrous Na 2 SO 4 It was dried for 1 h, filtered, and the filtrate was spin-dried and passed through the column to obtain 2.21 g of white solid (4b), with a yield of 75%.
[0056] Take 1.47g (3mmol) of compound (4b) and 1.24g (9mmol) of potassium carbonate into a 50ml round bottom flask, add 25ml redistilled DMF, slowly add 0.7ml (9mmol) of iodoethanol dropwise, and stir at 50°C for 8-12h . After the reaction, the reaction solution was diluted with 100ml of ethyl acetate, washed with water ...
Embodiment 3
[0061] Synthesis and characterization of compound 1c:
[0062]
[0063] Take compound (2c) 1.68g (6mmol), compound (3c) 0.85g (6mmol), HOBT 2.43g (18mmol), HBTU 6.83g (18mmol) into a 100ml round bottom flask, add redistilled DMF 40ml under nitrogen protection, Add DIPEA8.92ml (54mmol), and stir at room temperature for 4h. After the reaction, the reaction solution was diluted with 200ml of ethyl acetate, washed with water (50ml×5) to remove DMF, and the organic phase was washed with anhydrous Na 2 SO 4 It was dried for 1 h, filtered, and the filtrate was spin-dried and passed through the column to obtain 1.77 g of white solid (4c), with a yield of 73%.
[0064] Take 1.21g (3mmol) of compound (4c) and 1.24g (9mmol) of potassium carbonate into a 50ml round bottom flask, add 25ml redistilled DMF, slowly add iodopropanol 0.86ml (9mmol), and stir at 50°C for 12h. After the reaction, the reaction solution was diluted with 100ml of ethyl acetate (EA), washed with water (25ml×4) ...
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