Anti-infective drug and preparation method and application thereof
An anti-infection and drug technology, applied in the field of medicine, can solve the problems of drug toxicity and side effects
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Embodiment 1
[0079] Example 1: Preparation of 2-methyl-5-nitro-1-(((S)-oxiran-2-yl)methyl)1H-imidazole
[0080]
[0081] Weigh 100g of left-ornidazole and add it into 500ml of dichloromethane, stir and dissolve, cool down to -10~-15℃; weigh 36.5g of sodium hydroxide, add 500ml of water, stir and dissolve, let cool, slowly add dropwise into dichloromethane, Control the temperature not to exceed -10°C. After the addition, keep it warm at 0-5°C for 2 hours, separate the dichloromethane layer, extract the water layer with 100ml of dichloromethane, combine the dichloromethane layers, and add 100ml of water to the dichloromethane layer for washing. Twice, add an appropriate amount of anhydrous sodium sulfate to dry, filter, and concentrate the filtrate under reduced pressure to obtain 75.7 g of a brown oil.
Embodiment 2
[0082] Example 2: Preparation of 2-methyl-5-nitro-1-(((R)-oxiran-2-yl)methyl)1H-imidazole
[0083]
[0084] Weigh 100g of dex-ornidazole and add it into 500ml of dichloromethane, stir and dissolve, cool down to -10~-15°C; weigh 36.5g of sodium hydroxide, add 500ml of water, stir and dissolve, let it cool, and slowly add it dropwise into dichloromethane, Control the temperature not to exceed -10°C. After the addition, keep it warm at 0-5°C for 2 hours, separate the dichloromethane layer, extract the water layer with 100ml of dichloromethane, combine the dichloromethane layers, and add 100ml of water to the dichloromethane layer for washing. Twice, add an appropriate amount of anhydrous sodium sulfate to dry, filter, and concentrate the filtrate under reduced pressure to obtain 72.5 g of a brown oil.
Embodiment 3
[0085] Example 3: Preparation of 2-methyl-5-nitro-1-((oxiran-2-yl)methyl)1H-imidazole
[0086]
[0087] Weigh 100g of ornidazole and add it into 500ml of dichloromethane, stir and dissolve, cool down to -10~-15℃; weigh 36.5g of sodium hydroxide, add 500ml of water, stir and dissolve, let cool, slowly add dropwise into dichloromethane, control The temperature should not exceed -10°C. After the addition, keep it warm at 0-5°C for 2 hours, separate the dichloromethane layer, extract the water layer with 100ml of dichloromethane, combine the dichloromethane layers, and add 100ml of water to the dichloromethane layer to wash for 2 hours. Once, add an appropriate amount of anhydrous sodium sulfate to dry, filter, and concentrate the filtrate under reduced pressure to obtain 76.3 g of a brown oil.
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