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HRID 21213作成日:2026年10月24日

Water → 4-(4-Methoxyphenyl)-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone

https://huagongshe.com/ja/reaction/21213

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物Potassium CarbonateHCID 11430—
反応物(4-Methoxyphenyl)boronic acidHCID 201262—
反応物4-Trifluoromethanesulfonyloxy-7-(1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinoneHCID 86628286—
溶媒1,2-DimethoxyethaneHCID 8071—
生成物4-(4-Methoxyphenyl)-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinoneHCID 6849008671.4%

反応手順

In a similar manner to Step 1 of Example 152, 4-trifluoromethanesulfonyloxy-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (80.0 mg, 0.135 mmol) was dissolved in dimethoxyethane (5.6 mL), and the solution was added with 4-methoxyphenylboronic acid (62 mg, 0.41 mmol), [bis(diphenylphosphino)ferrocene]dichloropalladium (13.2 mg, 0.0166 mmol), potassium carbonate (93.0 mg, 0.675 mmol) and water (0.049 mL), followed by purification by preparative thin-layer chromatography (chloroform/methanol=8/1) to obtain 4-(4-methoxyphenyl)-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (53.2 mg, yield 71%).

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-02c8e221a3d04a2ca1b684325f604f07
出典メモuspto-grants-2010_06