A kind of preparation method of linezolid
A technology of linezolid and acetamide, which is applied in the field of preparation of antibacterial drugs, can solve the problems of high toxicity, more equipment required, and greater safety, and achieve the effects of high yield, low production cost, and few reaction steps
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example 1
[0018] (1) Under the protection of nitrogen, add 0.15 mol of acetamide and 100 ml of toluene to a 250 ml four-necked bottle, cool down to 0-5°C and add 0.12 mol of sodium amide in batches, slowly rise to room temperature and keep the reaction for 1 hour. Then the toluene was removed under reduced pressure, and the residue was the crude product of acetamide monosodium salt, which was set aside;
[0019] (2) Under nitrogen protection, add the crude acetamide monosodium salt prepared in the previous step to 200 grams of N,N-dimethylformamide, and then add R)-N-[3-(3-fluoro-( 4-morpholinyl)phenyl)-2-oxo-5-oxazolidinyl]methanol methanesulfonate 37.4 g (0.1 mol), kept at 50°C until HPLC detection R)-N-[3-(3 -Fluoro-(4-morpholinyl)phenyl)-2-oxo-5-oxazolidinyl]methanol mesylate None, the reaction is over, the reaction solution is cooled to 20°C, and the reaction solution is added to 1000 grams of water A large amount of off-white solid was precipitated, and after stirring for 1 hour,...
example 2
[0021] (1) Under the protection of nitrogen, add 0.15 mol of acetamide and 100 ml of toluene to a 250 ml four-necked bottle, cool down to 0-5°C and add 0.12 mol of lithium amide in batches, slowly rise to room temperature and keep the reaction for 1 hour. Then the toluene was removed under reduced pressure, and the residue was the crude product of acetamide monolithium salt, which was set aside;
[0022] (2), under the protection of nitrogen, add the crude acetamide monolithium salt prepared in the previous step to 200 grams of N,N-dimethylformamide, and then add R)-N-[3-(3-fluoro-( 4-morpholinyl)phenyl)-2-oxo-5-oxazolidinyl]methanol methanesulfonate 37.4 g (0.1 mol), reaction at 40 ° C until HPLC detection R)-N-[3-( 3-Fluoro-(4-morpholinyl)phenyl)-2-oxo-5-oxazolidinyl]methanol mesylate None, the reaction is over, the reaction solution is cooled to 20°C, and the reaction solution is added to 1000 g A large amount of off-white solids were precipitated in the water, and after c...
Embodiment 3
[0024] (1) Under the protection of nitrogen, add 0.15 mol of acetamide and 100 ml of toluene to a 250 ml four-necked bottle, cool down to 0-5°C and add 0.12 mol of metal potassium in batches, and slowly rise to room temperature for 1 hour after the addition is completed. Then the toluene was removed under reduced pressure, and the residue was the crude product of acetamide monopotassium salt, which was set aside;
[0025] (2), under the protection of nitrogen, add the crude acetamide monopotassium salt prepared in the previous step to 200 grams of N,N-dimethylformamide, and then add R)-N-[3-(3-fluoro-( 4-morpholinyl)phenyl)-2-oxo-5-oxazolidinyl]methanol methanesulfonate 37.4 g (0.1 mol), reaction at 50°C until HPLC detection R)-N-[3-( 3-Fluoro-(4-morpholinyl)phenyl)-2-oxo-5-oxazolidinyl]methanol mesylate None, the reaction is over, the reaction solution is cooled to 20°C, and the reaction solution is added to 1000 g A large amount of off-white solids were precipitated in the ...
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