Preparation method of Bilastine
A raw material, aqueous solution technology, applied in organic chemistry and other directions, can solve the problems of ether bond cleavage, difficult removal of impurities, difficult product purification, etc., and achieves the effects of mild reaction conditions, no side reactions, and simple operation.
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Embodiment 1
[0019] 5g 2-[1-(2-{4-[1-(4,4-dimethyl-4,5-dihydro-oxazol-2-yl)-1-methyl-ethyl]-benzene Base}-ethyl)-piperidin-4-yl]-1-(2-ethoxy-ethyl)-1H-benzimidazole was added to a clean three-neck flask, 150ml of 4N formic acid solution was added, and heated to reflux for 36 hours , adjusted to pH=7 with 10% aqueous sodium hydroxide solution, extracted with dichloromethane, and the solvent was spinned out to obtain a white solid with a yield of 90.5%.
Embodiment 2
[0021] 5g 2-[1-(2-{4-[1-(4,4-dimethyl-4,5-dihydro-oxazol-2-yl)-1-methyl-ethyl]-benzene Base}-ethyl)-piperidin-4-yl]-1-(2-ethoxy-ethyl)-1H-benzimidazole was added to a clean three-necked flask, 150ml of 4N trifluoroformic acid solution was added, and heated to reflux After 36 hours, adjust the pH to 7 with 10% aqueous sodium hydroxide solution, extract with dichloromethane, and spin out the solvent to obtain a white solid with a yield of 92.6%.
Embodiment 3
[0023] 5g 2-[1-(2-{4-[1-(4,4-dimethyl-4,5-dihydro-oxazol-2-yl)-1-methyl-ethyl]-benzene Base}-ethyl)-piperidin-4-yl]-1-(2-ethoxy-ethyl)-1H-benzimidazole was added to a clean three-neck flask, 150ml of 4N acetic acid solution was added, and heated to reflux for 36 hours , adjusted to pH=7 with 10% aqueous sodium hydroxide solution, extracted with dichloromethane, and the solvent was spinned out to obtain a white solid with a yield of 89.7%.
[0024]
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