Synthesis method of metamifop
A technology of oxazolam and a synthesis method, applied in the field of organic synthesis, can solve the problems of low product purity, high cost, and many three wastes, etc., and achieve the effects of high purity, mild conditions and high yield
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Embodiment 1
[0031] Add 333.7g (1mol) (R)-2-(4-((6-chlorobenzoxazole)oxy)phenoxypropionic acid (ee value: 99.6%) to a 2000mL four-neck flask under normal temperature and pressure 1000g dichloromethane, start stirring, add 162.1g (1mol) CDI in 5 batches within 30min, add 21.8g (0.1mol) ImTfOH, continue stirring at a temperature of 20°C for 1h.
[0032] Add 125.1g (1mol) N-methyl-o-fluoroaniline and 300g dichloromethane into a 2000mL four-necked flask, and drop (R)-2-(4-((6-chlorobenzoxazole) Oxygen) phenoxypropionic acid solution, control the dropping time at about 1 hour, control the temperature at 20°C during the dropping process, and stir and react at a temperature of 20°C for 2h after the dropping. After the reaction, the reaction solution is extracted with water 2 times, each time the water consumption was 200g, the organic phase was stripped of dichloromethane, and 422.4g of the oxafenamide product was obtained, the purity was 98.2%, the yield was 95.8%, and the ee value was 99.6%.
Embodiment 2
[0034] Add 333.7g (1mol) (R)-2-(4-((6-chlorobenzoxazole)oxy)phenoxypropionic acid (ee value: 99.6%) to a 2000mL four-neck flask under normal temperature and pressure 1000g acetonitrile, start stirring, add 162.1g (1mol) CDI in 5 batches within 30min, add 21.8g (0.1mol) ImTfOH, continue stirring at a temperature of 20°C for 1h.
[0035] Add 125.1g (1mol) of N-methyl-o-fluoroaniline and 300g of acetonitrile into a 2000mL four-necked flask, and drop (R)-2-(4-((6-chlorobenzoxazole)oxyl ) phenoxypropionic acid solution, control the dropping time at about 1 hour, control the temperature at 20°C during the dropping process, and stir and react at 20°C for 2h after the dropping is completed. After the reaction, extract 2 times from the reaction solution, 1000g of water and 1000g of dichloroethane were used for the first time, and the dichloroethane was removed from the organic phase to obtain 413.3g of the oxazifen product, with a purity of 96.3%, a yield of 93.7%, and an ee value of 9...
Embodiment 3
[0037] Add 333.7g (1mol) (R)-2-(4-((6-chlorobenzoxazole)oxy)phenoxypropionic acid (ee value: 99.6%) to a 2000mL four-neck flask under normal temperature and pressure 1000g dichloromethane, start stirring, add 162.1g (1mol) CDI in 5 batches within 30min, add 10.9g (0.05mol) ImTfOH, continue stirring at a temperature of 20°C for 1h.
[0038] Add 125.1g (1mol) N-methyl-o-fluoroaniline and 300g dichloromethane into a 2000mL four-necked flask, and drop (R)-2-(4-((6-chlorobenzoxazole) Oxygen) phenoxypropionic acid solution, control the dropping time at about 1 hour, control the temperature at 20°C during the dropping process, stir and react at 20°C for 2h after the dropping is completed. After the reaction, the reaction solution is extracted with water twice , the water consumption is 200g each time, and the dichloromethane is desorbed from the organic phase to obtain 418.6g of the oxapropen product, the purity is 97.6%, the yield is 94.9%, and the ee value is 99.6%.
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