反応 #42410

反応方程式

sodium borohydride

N-{(1S,2R)-1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl}-3-oxoindane-5-carboxamide

SP-201

→

title compound

N-{(1S,2R)-1-(3,5-Difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl}-3-hydroxyindane-5-carboxamide

溶媒

methanol

反応条件

後処理

1. 1
   濃縮The reaction is concentrated under reduced pressure
2. 2
   workup.DISSOLUTIONredissolved in water (3 mL)
3. 3
   その他partitioned into ethyl acetate
4. 4
   洗浄The organic layer is washed with water, saturated sodium bicarbonate, and brine
5. 5
   乾燥dried (sodium sulfate)
6. 6
   ろ過filtered
7. 7
   濃縮concentrated under reduced pressure

実験手順

To an ice-cold solution of N-{(1S,2R)-1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl}-3-oxoindane-5-carboxamide prepared by the method in Example SP-201 (66 mg, 0.13 mmol) in methanol (3 mL) is added sodium borohydride (20 mg, 0.52 mmol). The reaction stirred at room temperature 3 h. The reaction is concentrated under reduced pressure, redissolved in water (3 mL) and partitioned into ethyl acetate. The organic layer is washed with water, saturated sodium bicarbonate, and brine, dried (sodium sulfate), filtered, and concentrated under reduced pressure to give the title compound. ESI MS m/z 495.2 [M+H]+.

出典