反応 #41336

反応方程式

(1R,2S)-1-{[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy}-1-(3-methoxyphenyl)propan-2-amine

cyclopentanecarboxylic acid

→

N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-(3-methoxyphenyl)propan-2-yl]cyclopentanecarboxamide

溶媒

dichloromethane

dichloromethane

反応条件

後処理

1. 1
   その他to give a colorless solution
2. 2
   workup.WAITthe stirring was continued at r.t. overnight
3. 3
   その他The solvent was removed in vacuo
4. 4
   workup.DISSOLUTIONthe residue dissolved in acetonitrile/water mixture
5. 5
   その他the crude product purified by preparative HPLC

実験手順

To a stirred solution of 1,1-carbonyldiimidazole (12 mg, 70 μmol) in dichloromethane (1 ml) was added cyclopentanecarboxylic acid (11 μl, 100 μmol) to give a colorless solution. The reaction mixture was stirred for 1 h at r.t. Then a solution of (1R,2S)-1-{[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy}-1-(3-methoxyphenyl)propan-2-amine (6a, 19 mg, 50 μmol) in dichloromethane (0.5 ml) was added, and the stirring was continued at r.t. overnight. The solvent was removed in vacuo, the residue dissolved in acetonitrile/water mixture, and the crude product purified by preparative HPLC. Yield 18 mg (76%).

出典