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HRID 21016作成日:2026年10月24日

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

https://huagongshe.com/ja/reaction/21016

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EthanolamineHCID 700—
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-[(2-hydroxyethyl)aminomethyl]indol-2-yl)isoindolinoneHCID 6849348788.7%

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 (40.0 mg, 0.0974 mmol) was dissolved in acetonitrile (2 mL), and the solution was treated with 2-aminoethanol (0.024 mL, 0.39 mmol), acetic acid (0.112 mL, 1.96 mmol) and sodium triacetoxyborohydride (103 mg, 0.486 mmol), followed by purification by preparative thin-layer chromatography (hexane/ethyl acetate=1/2) to obtain 4-chloro-7-(1-(tert-butoxycarbonyl)-5-[(2-hydroxyethyl)aminomethyl]indol-2-yl)isoindolinone (39.4 mg, yield 871).

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-73bf989f857b4d09be8e831772c26208
出典メモuspto-grants-2010_06