反応 #2358577

反応方程式

H2O

compound 25

2-(6-(4-(4-fluorophenoxy)phenyl)pyridin-2-yl)acetic acid

(L)-Ala-OMe

DCC

→

compound 26

収率 81.0%

2-{6-[4-(4-fluoro-phenoxy)phenyl]-pyridin-2-yl}-acetylamino-propionic acid methyl ester

収率 81.0%

溶媒

DCM

Hexane

EtOAc

DCM

反応条件

後処理

1. 1
   その他The organic phase was separated
2. 2
   乾燥dried over anhydrous Na2SO4
3. 3
   その他The solvent was removed
4. 4
   その他the residue was purified by the preparative TLC (MeOH

実験手順

To a solution of compound 25 (30 mg, 0.1 mol) in DCM (1 mL) was added (L)-Ala-OMe (10.3 mg, 0.1 mmol), DCC (23.7 mg, 0.12 mmol) and DMAP (1.2 mg, 0.01 mmol). The reaction mixture was stirred overnight at room temperature. After the reaction was complete, H2O (1 mL) was added. The organic phase was separated and dried over anhydrous Na2SO4. The solvent was removed and the residue was purified by the preparative TLC (MeOH:DCM=1:9, then EtOAc:Hexane=2:1) to give compound 26 (2 mg, 81% yield, LC/MS: m/z=409 [M+H]+, 1H NMR (400 MHz, CD3OD): δ 8.04 (d, J=8.8 Hz, 2H), 7.81 (t, J=7.8 Hz 1H), 7.7 (d, J=7.2 Hz, 1H), 7.31 (d, J=7.0 Hz, 1H), 7.03-7.1 (m, 6H), 4.47 (q, J=7.3 Hz, 1H), 3.83 (s, 2H), 3.71 (s, 3H), 1.42 (d, J=7.2 Hz, 3H)).

出典