反应详情

温度

27.5 °C

Methyl 5-aminobenzofuran-2-carboxylate (200 g) and N-benzenesulfonyl-N,N-bis(2-chloroethyl)amine (289 g) were added to tributyl amine (1012 ml) under stirring at 25-30° C. The resulting mixture was heated to 73-77° C., followed by stirring for 43 hours at the same temperature. The reaction mass was cooled to 25-30° C., followed by the addition of methanol (506 ml) and then stirring for 30 minutes at 25-30° C. The resulting mass was filtered, washed with chilled methanol (200 ml) and then dried to produce 220 g of methyl 5-[4-(benzenesulfonyl)-1-piperazinyl]benzofuran-2-carboxylate as a fine powder (Purity by HPLC: 99.5%).

1. temperatureThe resulting mixture was heated to 73-77° C.
2. stirringby stirring for 43 hours at the same temperature
3. temperatureThe reaction mass was cooled to 25-30° C.
4. stirringstirring for 30 minutes at 25-30° C
5. filtrationThe resulting mass was filtered
6. washwashed with chilled methanol (200 ml)
7. customdried