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HRID 561578作成日:2026年10月27日

Trifluoroacetic acid → 3-[1-Cyclopropyl-1-(4-fluorophenyl)ethyl]-7-[(methylsulfanyl)methyl]-1H-indole

https://huagongshe.com/reaction/561578

反応式

関与物質

役割名称HCID仕込み量
反応物Trifluoroacetic acidHCID 6422—
反応物1-Cyclopropyl-1-(4-fluorophenyl)ethanolHCID 98104—
反応物7-[(Methylsulfanyl)methyl]-1H-indoleHCID 58392187—
溶媒DichloromethaneHCID 6344—
生成物3-[1-Cyclopropyl-1-(4-fluorophenyl)ethyl]-7-[(methylsulfanyl)methyl]-1H-indoleHCID 58392106—

反応手順

559 mg (3.10 mmol) of the compound from Example 77A and 0.26 ml (3.39 mmol) of trifluoroacetic acid were added to 500 mg (2.82 mmol) of the compound from Example 8A in 12 ml of dichloromethane. The reaction mixture was stirred at RT for 30 min and then diluted with dichloromethane, washed with saturated aqueous sodium bicarbonate solution and saturated aqueous sodium chloride solution, dried over sodium sulfate, filtered and concentrated. Purification of the crude product by preparative HPLC (mobile phase: acetonitrile/water gradient) resulted in 361 mg (38% of theory) of the title compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08063234B2
出典データセットuspto-grants-2011_11
ORD IDord-0be2306708914b3e9eb50432c2e77ae8
出典メモuspto-grants-2011_11