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HRID 1854784作成日:2026年10月25日

Water → Ambrisentan

https://huagongshe.com/reaction/1854784

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物4,6-Dimethyl-2-methylsulfonylpyrimidineHCID 2772382—
反応物Potassium tert-butoxideHCID 23665647—
反応物(R)-2,4-dichlorophenylethyl ammonium (S)-2-hydroxy-3-methoxy-3,3-diphenylpropionateHCID 86668129—
溶媒DimethylformamideHCID 6228—
生成物AmbrisentanHCID 6918493—

反応手順

In a 25 mL three neck flask with stirring arrangement, (1 gm) (R)-2,4-dichlorophenylethyl ammonium (S)-2-hydroxy-3-methoxy-3,3-diphenylpropionate and (0.726 gm) potassium tertiary butoxide (6.488 mmol) in 10 ml DMF at 25° C. were taken and stirred for 5 min. (0.604 gm) 4,6-dimethyl-2-(methylsulfonyl)pyrimidine (3.244 mmol) was added to the reaction mixture in one lot. The reaction mixture was stirred at room temperature for 6 hours and subsequently dumped into cold water and washed the aqueous layer with toluene. Aqueous layer was collected and acidified with HCl to pH 2. The solid was extracted with ethyl acetate, and wash the ethyl acetate layer with water followed by brine. Dry over sodium sulphate and concentrated on Buchi Rotavapor.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08962832B2
出典データセットuspto-grants-2015_02
ORD IDord-cfa0838c16104336aac10dcfe2d00eec
出典メモuspto-grants-2015_02