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HRID 348756作成日:2026年10月24日

Phthalimide → 2-[2-(4-dipropylaminobutyl)-3-propyl-3H-benzimidazol-5-ylmethyl]isoindole-1,3-dione

https://huagongshe.com/ja/reaction/348756

反応式

関与物質

役割名称HCID仕込み量
反応物PhthalimideHCID 6809—
反応物TriphenylphosphineHCID 11776—
反応物[2-(4-dipropylaminobutyl)-3-propyl-3H-benzimidazol-5-yl]methanolHCID 23079221—
反応物Diethylazodicarboxylate tolueneHCID 66777355—
溶媒TolueneHCID 1140—
生成物2-[2-(4-dipropylaminobutyl)-3-propyl-3H-benzimidazol-5-ylmethyl]isoindole-1,3-dioneHCID 2315550141.9%

反応条件

温度0 °C

反応手順

The compound (302 mg) obtained in Example 125-4 was dissolved in toluene (6.0 ml) and added with triphenylphosphine (275 mg) and phthalimide (193 mg), followed by cooling to 0° C. In this solution, a 40% diethyl azodicarboxylate/toluene solution (452 mg) was dropped. After that, the solution was stirred overnight at room temperature. After completion of the reaction, the solvent was distilled off under reduced pressure. The residue was dissolved in chloroform and washed with water. Then, the solution was subjected to extraction with chloroform and the extract was then washed with saturated saline solution. The organic layer was dried with anhydrous sodium sulfate. After filtration, the solvent was distilled off under reduced pressure and the residue was then purified through silica gel column chromatography (chloroform/methanol), thereby obtaining the subject compound (174 mg) as a pale-yellow solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07176227B2
出典データセットuspto-grants-2007_02
ORD IDord-b38b06ee95044a93b17e6cf98e20a304
出典メモuspto-grants-2007_02