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HRID 248作成日:2026年10月23日

Benzylamine → 6-benzylamino-3,4-dihydro-2H-isoquinolin-1-one

https://huagongshe.com/ja/reaction/248

反応式

関与物質

役割名称HCID仕込み量
反応物BenzylamineHCID 7504—
反応物6-Bromo-3,4-dihydro-2H-isoquinolin-1-oneHCID 21865450—
試薬Potassium tert-butoxideHCID 23665647—
触媒Binap, (A+-)-HCID 634876—
触媒Palladium (II) acetateHCID 4144353—
生成物6-benzylamino-3,4-dihydro-2H-isoquinolin-1-oneHCID 672239150%

反応条件

温度130 °C

反応手順

**Repeat 02915-84 but use NO solvent** In a 5 mL sealed MW* test tube was 6-bromo-3,4-dihydroisoquinolin-1(2H)-one (50 mg, 0.22 mmol), phenylmethanamine (97 µl, 0.88 mmol), BINAP (6.89 mg, 0.01 mmol) and palladium(II) acetate (2.483 mg, 0.01 mmol) combined to give a tan suspension. potassium tert-butoxide (24.82 mg, 0.22 mmol) was then added last. Placed test tube onto Smith MW* platform. Heated reaction to 70°C for 5 minutes. NO reaction!!! Added DMF (0.5 ml) and reheated reaction to 130°C for 15 mins. Took LCMS - no reaction, only unreacted SM!! Discarded reaction.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-4a6bd61cd0ff477baa0ad5e567d741e9
出典メモ750 AstraZeneca ELN dataset