反応 #71459

反応方程式

8-(2-chloro-6-fluoro-3,5-dimethoxy-phenyl)-quinoxaline-5-carboxylic acid ethyl ester

4-(6-amino-pyridin-3-ylmethyl)-piperazin-2-one

NaHCO3

trimethyl aluminum

→

title compound

8-(2-Chloro-6-fluoro-3,5-dimethoxy-phenyl)-quinoxaline-5-carboxylic acid [5-(3-oxo-piperazin-1-ylmethyl)-pyridin-2-yl]amide

溶媒

DCM

DCM MeOH

反応条件

後処理

1. 1
   その他The title compound was prepared in analogy to the procedure

実験手順

The title compound was prepared in analogy to the procedure described in Example 115 but using 8-(2-chloro-6-fluoro-3,5-dimethoxy-phenyl)-quinoxaline-5-carboxylic acid ethyl ester (Step 144.1), 4-(6-amino-pyridin-3-ylmethyl)-piperazin-2-one (Step 103.1), 2 equiv of trimethyl aluminum, stirring the reaction mixture for 6 h at 80° C., pouring it onto a saturated aqueous solution of NaHCO3 and DCM. The title compound: ESI-MS: 551.0 [M+H]+; tR=3.59 min (System 1); TLC: Rf=0.13 (DCM/MeOH/NH3aq, 94:5:1).

出典