反応 #49172

反応方程式

Compound 4a

(6-{2-[Bis-(4-methoxy-phenyl)-phenyl-methoxymethyl]-4-hydroxy-pyrrolidin-1-yl}-6-oxo-hexyl)-carbamic acid benzyl ester

→

compound 5

収率 91.4%

6-Amino-1-{2-[bis-(4-methoxy-phenyl)-phenyl-methoxymethyl]-4-hydroxy-pyrrolidin-1-yl}-hexan-1-one

収率 91.4%

溶媒

ethyl acetate

反応条件

後処理

1. 1
   その他purged with argon
2. 2
   workup.ADDITIONTo the solution was added 10% palladium on carbon (2 g)
3. 3
   その他The flask was purged with hydrogen 2 times
4. 4
   ろ過The reaction mixture was filtered through a pad of Celite
5. 5
   洗浄washed with ethyl acetate
6. 6
   濃縮The combined organic layer was concentrated under reduced pressure

実験手順

Compound 4a (14.5 g, 21.7 mmol) was dissolved in ethyl acetate (100 mL) and purged with argon. To the solution was added 10% palladium on carbon (2 g). The flask was purged with hydrogen 2 times and stirred further at room temperature under hydrogen atmosphere for overnight. The disappearance of the starting material was confirmed by the TLC. The reaction mixture was filtered through a pad of Celite and washed with ethyl acetate. The combined organic layer was concentrated under reduced pressure to afford compound 5 (10.56 g, 91%) as white solid. This was used as such for the next step.

出典