反应详情

0.5 g (1.53 mmole) of ethyl α-[2-chloro-4-(2,3,4,5-tetrahydro-5-methyl-3-oxo-1,2,4-triazin-6-yl)phenoxy]acetate (prepared as described in Example 5) was mixed with 0.58 g (3.06 mmole) of 4-amino-1-benzylpiperidine, and the mixture was stirred at 120°-130° C. for 2.5 hours. The mixture was then cooled, after which it was subjected to column chromatography through silica gel and eluted with methylene chloride containing 2% v/v ethanol to give 0.5 g of a pale yellow oil. Trituration of this oil with ethanol yielded crystals, which were then recrystallized from ethanol, to give 0.33 g of the title compound as pale yellow fine crystals melting at 190°-191° C.

1. temperatureThe mixture was then cooled
2. washeluted with methylene chloride containing 2% v/v ethanol