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HRID 21014作成日:2026年10月23日

Acetic Acid → 4-Chloro-7-(1-(tert-butoxycarbonyl)-5-[di(2-hydroxyethyl)aminomethyl]indol-2-yl)isoindolinone

https://huagongshe.com/ja/reaction/21014

反応式

関与物質

役割名称HCID仕込み量
反応物Acetic AcidHCID 176—
反応物DiethanolamineHCID 8113—
反応物Sodium triacetoxyborohydrideHCID 5049666—
反応物4-Chloro-7-[1-(tert-butoxycarbonyl)-5-formylindol-2-yl]isoindolinoneHCID 86628227—
溶媒AcetonitrileHCID 6342—
生成物4-Chloro-7-(1-(tert-butoxycarbonyl)-5-[di(2-hydroxyethyl)aminomethyl]indol-2-yl)isoindolinoneHCID 6849086064%

反応手順

In a similar manner to Step 2 of Example 6, 4-chloro-7-[1-(tert-butoxycarbonyl)-5-formylindol-2-yl]isoindolinone (37.6 mg, 0.0922 mmol) was dissolved in acetonitrile (2 mL), and the solution was treated with diethanolamine (0.035 mL, 0.37 mmol), acetic acid (0.106 mL, 1.85 mmol) and sodium triacetoxyborohydride (98 mg, 0.46 mmol), followed by purification by preparative thin-layer chromatography (hexane/ethyl acetate=1/2) to obtain 4-chloro-7-(1-(tert-butoxycarbonyl)-5-[di(2-hydroxyethyl)aminomethyl]indol-2-yl)isoindolinone (29.2 mg, yield 64%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07745641B2
出典データセットuspto-grants-2010_06
ORD IDord-ef82224e0ab342b3b88883e0807733d5
出典メモuspto-grants-2010_06