3-aryl-7H-thiazol[3,2-b]-1,2,4-triazinyl-7-one derivatives and application thereof
A CH2, drug technology, applied in the field of medicine, can solve problems such as drug resistance or pharmacokinetic deficiencies
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Embodiment 1
[0032] Preparation of 2-methyl-4-methylenethienoxazolone
[0033] Add 0.1 mol of 2-thiophene carboxaldehyde, 0.12 mol of acetylglycine, 0.12 mol of anhydrous sodium acetate and 50 grams of acetic anhydride into a 100-degree three-necked flask in sequence, heat and reflux and stir for 5 hours to react. After cooling to room temperature, the solution becomes solid. Suction filtration, the filter cake was washed with cold water, and recrystallized with acetone to obtain 19.3 g of the desired product as a yellow crystalline powder with a yield of 100% and MS m / z (M) 193.
Embodiment 2
[0035] Preparation of α-Acetamido-β-thiophene Acrylic Acid
[0036] Add 0.1mol of 2-methyl-4-methylenethienoxazolone compound, 100mL of water, and 80mL of acetone into a 100mL round-bottomed flask in sequence, heat to reflux and stir for 3 hours, cool to room temperature, and a large number of yellow solids are precipitated. After suction filtration, the filter cake was rinsed with cold water and a small amount of acetone, and recrystallized with acetone to obtain 20.3 g of the desired product as yellow crystals, with a yield of 96.2 and MS m / z (M) 211.
Embodiment 3
[0038] Preparation of β-thienylpyruvate
[0039]Add 0.1mol of α-acetylamino-β-thiophene acrylic acid, 60mL of 1mol / L HCl solution into a 100mL round-bottomed flask, heat and reflux for 1 hour, stop the reaction, filter while it is hot, and solids precipitate out of the filtrate. Cooling, suction filtration, recrystallization from absolute ethanol to obtain 15.5 g of the desired product red crystals, yield 91.2%, MS m / z (M) 170.
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