Alpha-glucosidase inhibitor, and synthesis method and application thereof
A technology of glucosidase and synthesis method, which is applied in the field of α-glucosidase inhibitor and its synthesis, and achieves the effects of good inhibitory activity and good application prospect
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[0048] Example 1
[0049] Synthesis of 1,2,4,5-Tetramethoxybenzene (Intermediate A)
[0050]
[0051]2,5 dihydroxy-1,4 benzoquinone (5 g, 3.6 mmol) was dissolved in 200 mL of methanol solution, 38% concentrated hydrochloric acid (6 mL, 72.0 mmol) was slowly added, and the mixture was stirred at room temperature overnight. After the completion of the reaction (TLC), suction filtration was concentrated to obtain a yellow solid intermediate product 1; the obtained intermediate product 1 was dissolved in 50 mL of water, sodium dithionite (10 g, 57.4 mmol) was added, and at 120 ° C, the reaction was refluxed for 8 minutes, at- Crystallization by cooling at 4°C, and the mixture was filtered with suction to obtain intermediate product 2 (4.5 g, 73.5%) in the form of powder white crystals; Intermediate product 2 (1.7 g, 10 mmol) was dissolved in 10 mL of DMSO, potassium hydroxide (1.4 g, 25 mmol), stirred at room temperature for 15 minutes, added iodomethane (1.88 mL, 25 mmol) dro...
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[0053] Example 2
[0054] Synthesis of 1,2,4,5-Tetramethoxy-3-(7-phenylheptyl)-benzene (Intermediate B1)
[0055]
[0056] Intermediate A (1 g, 5.1 mmol) was added to a round-bottomed flask, dried in vacuo for 30 minutes, added with HMPA (353 μL, 2 mmol), ventilated 2 to 5 times, and then added 60 mL of tetrahydrofuran as solvent. The water was reacted without oxygen for 15 minutes, n-butyllithium (2.44 mL, 6.12 mmol) was slowly added, the temperature was adjusted to -10 °C for 1 hour, 1-bromo-7-phenylheptane was added dropwise, and the reaction was continued for 10 minutes . The mixture was then left to react at room temperature for 10 hours. After the reaction solution was concentrated under reduced pressure, it was dissolved in an organic solvent, and the saturated ammonium chloride solution was adjusted to pH 5 to 6. The organic phase was washed with distilled water and saturated brine, respectively. The organic phase was collected and dried with anhydrous magnesium s...
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[0065] Example 3
[0066] Synthesis of 1,2,4,5-Tetramethoxy3-(2-cyclohexylethyl)benzene (Intermediate B2)
[0067]
[0068] Intermediate A (1 g, 5.1 mmol) was added to a round-bottomed flask, dried in vacuo for 30 minutes, added with HMPA (353 μL, 2 mmol), ventilated 2 to 5 times, and then added 60 mL of tetrahydrofuran as solvent. Water was reacted without oxygen for 15 minutes, n-butyllithium (2.44 mL, 6.12 mmol) was slowly added, the temperature was adjusted to -10° C. for 1 hour, 2-bromoethylcyclohexane was added dropwise, and the reaction was continued for 10 minutes. The mixture was then left to react at room temperature for 10 hours. After the reaction solution was concentrated under reduced pressure, it was dissolved in an organic solvent, and the saturated ammonium chloride solution was adjusted to pH 5 to 6. The organic phase was washed with distilled water and saturated brine, respectively. The organic phase was collected and dried with anhydrous magnesium sulfa...
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