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HRID 1432263作成日:2026年10月27日

Ammonium Chloride → (1-(4-Fluorobenzyl)-5-methanesulfonylindol-2-yl)(thiazol-2-yl)-methanol

https://huagongshe.com/reaction/1432263

反応式

関与物質

役割名称HCID仕込み量
反応物Ammonium ChlorideHCID 25517—
反応物2-BromothiazoleHCID 76430—
反応物1-(4-Fluorobenzyl)-5-methanesulfonylindole-2-carbaldehydeHCID 22504374—
反応物ButyllithiumHCID 178418339—
溶媒TetrahydrofuranHCID 8028—
溶媒HexaneHCID 8058—
生成物(1-(4-Fluorobenzyl)-5-methanesulfonylindol-2-yl)(thiazol-2-yl)-methanolHCID 2250445128.6%

反応手順

To a mixture of 2-bromothiazole (123 mg) and tetrahydrofuran (3.5 ml), 1.61 M n-butyl lithium solution in hexane (0.51 ml) was added at −78° C. and the mixture was stirred for 30 minutes, followed by addition of a solution of 1-(4-fluorobenzyl)-5-methanesulfonylindole-2-carbaldehyde (50 mg) obtained in Example 27 (4) in tetrahydrofuran (3.5 ml) at the same temperature, and the mixture was stirred as such for 30 minutes. The reaction mixture was poured into a saturated aqueous ammonium chloride solution, extracted with chloroform, washed with water, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was subjected to silica gel preparative thin-layer chromatography (hexane:ethyl acetate=1:1) to obtain 18 mg of the desired product as a yellow oil.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07612070B2
出典データセットuspto-grants-2009_11
ORD IDord-a1f24ac8428a4affa5a6823a6e025d62
出典メモuspto-grants-2009_11