Industrialization method for preparing tamoxifen citrate polycrystalline type A
A citric acid and polymorphic technology, applied in the field of medicinal chemistry, can solve problems such as difficult realization, increased impurities, and difficult industrialization
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Embodiment 1
[0045] The preparation of embodiment 1 tamoxifen citrate crystal form A:
[0046] Add 10.00 g of the crystal form of tamoxifen citrate into DMF (20ml), heat to dissolve at 60°C, and then slowly add it to xylene (200ml) pre-cooled at -20°C, at -10±5°C, After continuing to stir for 2-3 hours, filter, wash with a small amount of DMF:xylene (1:10), and dry at 60°C to obtain about 9.41g of polymorph A of tamoxifen citrate, mp: 143-145°C, HPLC 99.85%, maximum simple 0.05%, HPLC: 99.72%.
Embodiment 2
[0047] The preparation of embodiment 2 tamoxifen citrate crystal form A:
[0048] Add 10.00g of tamoxifen citrate to DMF (15ml), heat to dissolve at 60°C, then add it to pre-cooled toluene (200ml) with stirring, continue to stir at -10±5°C for 2 hours, then filter , washed with a small amount of DMF:toluene (1:10), and dried at 60°C to obtain about 9.28g of polymorph A of tamoxifen citrate, mp: 143-145°C.
Embodiment 3
[0049] The preparation of embodiment 3 tamoxifen citrate crystal form A:
[0050] Add 10.00g of tamoxifen citrate methanol solvate into DMF (15ml), heat to dissolve at 60°C, then add it to pre-cooled xylene (200ml) with stirring, and continue stirring at -10±5°C After 2 hours, filter, wash with a small amount of xylene, and dry at 60°C to obtain about 9.05 g of polymorph A of tamoxifen citrate, mp: 143-145°C.
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