Bilastine crystal and preparation method thereof
A crystal form, benzodiimazole technology, applied in the field of medicine, achieves good stability and is not easy to crystallize.
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[0015] Example one
[0016] 1.0 g of 4-[2-[1-(2-ethoxyethyl)-1H-benzodiazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethyl Phenylacetic acid was added to 8ml methanol, heated to dissolve, refluxed for one hour, naturally cooled to crystallize, filtered, and dried under vacuum at 50°C for 10 hours to obtain 0.72 g of 4-[2-[1-(2-ethoxyethyl) -1H-Benzodimazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethylphenylacetic acid new crystal form, yield 72%, measured melting point 197-200℃ .
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[0017] Implementation example two
[0018] Add 2.0 g of 4-[2-[1-(2-ethoxyethyl)-1H-benzodimazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethyl Phenylacetic acid was added to 16ml of toluene, heated to dissolve, the temperature was kept at about 70℃, kept for one hour, naturally cooled to crystallize, filtered, and dried under vacuum at 50℃ for 10 hours to obtain 1.5 g of 4-[2-[1-(2 -Ethoxyethyl)-1H-Benzodimazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethylphenylacetic acid new crystal form, yield 75%, measured The melting point is 197.5-200.2°C.
Example Embodiment
[0019] Implementation example three
[0020] 1.5 g of 4-[2-[1-(2-ethoxyethyl)-1H-benzodiazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethyl Phenylacetic acid was added to 14ml ethyl acetate, heated to dissolve, the temperature was kept at about 65℃, kept for one hour, naturally cooled to crystallize, filtered, and dried under vacuum at 50℃ for 10 hours to obtain 1.0 g of 4-[2-[1- (2-Ethoxyethyl)-1H-Benzodimazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethylphenylacetic acid new crystal form, yield 66.7% , The measured melting point is 197.5-199.8°C.
[0021] Attached figure 1 X-powder diffraction pattern of bilastine crystal form
[0022] Degree 2θ d-spacing Relative Strength(%) 9.27179.5469.73 10.90048.1135.37 12.74616.9453.88 15.66175.6545.34 17.68905.01100.00 18.32024.8464.71 20.03764.4377.25 21.90214.0552.89 27.35183.2626.65
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