反応 #8337

反応方程式

4-[2-(6-methyl-pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]-quinoline-7-carboxylic acid

(2-amino-2-methyl-propyl)-carbamic acid tert-butyl ester

EDC

1-hydroxybenzotriazole

N,N-diisopropylethylamine

→

title compound

収率 91.0%

[2-Methyl-2-({4-[2-(6-methyl-pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]-quinoline-7-carbonyl}-amino)-propyl]-carbamic acid tert-butyl ester

収率 91.0%

溶媒

dichloromethane

反応条件

後処理

1. 1
   濃縮concentrated in vacuo
2. 2
   洗浄washed with water and saturated aqueous sodium chloride
3. 3
   乾燥dried over sodium sulfate
4. 4
   濃縮concentrated in vacuo
5. 5
   その他The residue is chromatographed on SiO2 (methanol/dichloromethane/2:98)

実験手順

To a solution of 4-[2-(6-methyl-pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]-quinoline-7-carboxylic acid (0.16 g, 0.43 mmol), (2-amino-2-methyl-propyl)-carbamic acid tert-butyl ester (0.09 g, 0.47 mmol), EDC (0.09 g, 0.47 mmol), 1-hydroxybenzotriazole (0.06 g, 0.47 mmol) in dichloromethane (8.6 mL) is added N,N-diisopropylethylamine (0.25 mL, 1.29 mmol). The mixture is stirred at room temperature for 18 hand concentrated in vacuo. The residue is taken up in ethyl acetate, washed with water and saturated aqueous sodium chloride, dried over sodium sulfate and concentrated in vacuo. The residue is chromatographed on SiO2 (methanol/dichloromethane/2:98) to yield the title compound 0.21 g (91%) as a white solid.

出典