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HRID 571278作成日:2026年10月25日

Triethylamine → tert-butyl 2-(4-(N-(methylsulfonyl)methylsulfonamido)-1,3-dioxoisoindolin-2-yl)acetate

https://huagongshe.com/reaction/571278

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物Methanesulfonyl chlorideHCID 31297—
反応物Tert-butyl 2-(4-amino-1,3-dioxoisoindolin-2-yl)acetateHCID 86681685—
溶媒DichloromethaneHCID 6344—
生成物tert-butyl 2-(4-(N-(methylsulfonyl)methylsulfonamido)-1,3-dioxoisoindolin-2-yl)acetateHCID 8951191786%

反応手順

A mixture of tert-butyl 2-(4-amino-1,3-dioxoisoindolin-2-yl)acetate (712 mg, 2.58 mmol), triethylamine (1029 μl, 7.73 mmol) and methanesulfonyl chloride (602 μl, 7.73 mmol) in 20 ml of DCM was stirred overnight at room temperature. The mixture was washed with 1N HCl, brine and finally dried over sodium sulfate and evaporated; the residue was purified by flash chromatography (Hexane/EtOAc 3/1 to 1/1) yielding tert-butyl 2-(4-(N-(methylsulfonyl)methylsulfonamido)-1,3-dioxoisoindolin-2-yl)acetate as an off-white foam (0.96 g, 2.220 mmol, 86% yield, MS/ESI+ 454.8 [MNa]+) and used in the following reaction without further purification.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09024027B2
出典データセットuspto-grants-2015_05
ORD IDord-8fb56a23a70c47178497a89eee1d70ef
出典メモuspto-grants-2015_05