反応 #76849

反応方程式

1-[(3,4-Dimethoxy-benzyl)-6,7-dimethoxy-1,2,3,4-tetrahydro-naphthalen-2-yl]-phenyl-acetic acid

PyBOP

1-aminoindane

diisopropylethylamine

AcOEt

→

title compound

収率 64.0%

2-[1-(3,4-Dimethoxy-benzyl)-6,7-dimethoxy-1,2,3,4-tetrahydro-naphthalen-2-yl]-N-indan-1-yl-2-phenyl-acetamide

収率 64.0%

溶媒

CH2Cl2

DMF

反応条件

後処理

1. 1
   その他The mixture reaction
2. 2
   洗浄washed with water
3. 3
   抽出The aqueous phase was extracted twice with CH2Cl2
4. 4
   乾燥the combined organic extracts were dried over MgSO4
5. 5
   ろ過filtered
6. 6
   濃縮concentrated
7. 7
   その他to give a crude brown residue

実験手順

To a solution of 1-[(3,4-Dimethoxy-benzyl)-6,7-dimethoxy-1,2,3,4-tetrahydro-naphthalen-2-yl]-phenyl-acetic acid (100 mg, 0.209 mmol) in 5 ml of dry DMF, were added PyBOP (109 mg, 0.209 mmol), 1-aminoindane (32.3 mg, 0.19 mmol) and dropwise diisopropylethylamine (Hünig's base). (75 μl, 0.437 mmol). The mixture reaction was stirred at RT under argon for 20 h. The mixture was then dissolved in CH2Cl2 and washed with water. The aqueous phase was extracted twice with CH2Cl2, the combined organic extracts were dried over MgSO4, filtered and concentrated to give a crude brown residue. Flash chromatography (AcOEt) gave 72 mg (64%) of the title compound as a pale brown oil.

出典