反応 #466374

反応方程式

4-piperidone monohydrate hydrochloride

sodium bicarbonate

4-bromo-but-2-enoic acid[4-(3-chloro-4-fluoro-phenylamino)-3-cyano-7-methoxy-quinolin-6-yl]-amide

→

4-(4,4-Dihydroxy-piperidin-1-yl)-but-2-enoic Acid[4-(3-chloro-4-fluoro-phenylamino)-3-cyano-7-methoxy-quinolin-6-yl]-amide

溶媒

dimethylformamide

反応条件

後処理

1. 1
   その他The crude product was purified in the same manner as Example 117
2. 2
   その他produced 192 mg

実験手順

After the procedure of Example 117, 4-bromo-but-2-enoic acid[4-(3-chloro-4-fluoro-phenylamino)-3-cyano-7-methoxy-quinolin-6-yl]-amide. (0.51 mmol.) was stirred in dimethylformamide with 4-piperidone monohydrate hydrochloride (470 mg., 3.06 mmol.), and sodium bicarbonate (386 mg., 4.59 mmol.), for 24 hours. The crude product was purified in the same manner as Example 117 and produced 192 mg. (72%) of the product as a yellow solid: mp 225-30° C.

出典