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HRID 578743作成日:2026年10月26日

Water → Rosuvastatin

https://huagongshe.com/reaction/578743

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物ButylamineHCID 8007—
反応物Rosuvastatin n-butylamideHCID 86699893—
溶媒IsopropanolHCID 3776—
生成物RosuvastatinHCID 446157102.4%

反応条件

温度120 °C

反応手順

An autoclave having 800 cm3 is charged with 16.1 g (0.03 mol) rosuvastatin n-butylamide, 644 cm3 of water and 43.9 g (63.3 cm3; 0.60 mol) of n-butylamine. The reaction mixture is stirred at 120° C. for 24 hours, allowed to cool, diluted with 2-propanol at room temperature and evaporated in vacuo. The residue is boiled in ethylacetate, and while stirring, allowed to cool to room temperature. The crystals are filtered. Thus 14.8 g (89%) of rosuvastatin NBA salt are obtained. The crude salt is stirred in ethylacetate at room temperature, filtered, washed and dried. Thus dried product is boiled in ethylacetate, thereafter stirred in the same solvent at room temperature, filtered, washed and dried. Yield 9.32 g (56%) of rosuvastatin NBA salt, having purity (as determined by HPLC) exceeding 99.5%.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09040696B2
出典データセットuspto-grants-2015_05
ORD IDord-b9f9d6028af0454a98728bba3a69a714
出典メモuspto-grants-2015_05