Reaktion #466374

Reaktionsgleichung

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

Lösungsmittel

dimethylformamide

Reaktionsbedingungen

Aufarbeitung

1. 1
   SonstigeThe crude product was purified in the same manner as Example 117
2. 2
   Sonstigeproduced 192 mg

Vorschrift

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.

Quelle