反応 #8278

反応方程式

ethyl acetate

intermediate

3-(4-(1-(2(S),3-Dihydroxypropanoyl)-1,2,5,6-tetrahydropyrid-4-yl)-3,5-difluorophenyl)-5(S)-pyrazin-2-ylaminomethyloxazolidin-2-one

3-(t-butoxycarbonylamino)pyridazine

pyrazine

→

desired product

4-(1-(2,2-Dimethyl-1,3-dioxolan-4(S)-ylcarbonyl)-1,2,5,6-tetrahydropyrid-4-yl)-3,5-difluorophenyl-5(R)-(N-(t-butoxycarbonyl)pyridazin-3-ylaminomethyl)oxazolidin-2-one

溶媒

dichloromethane

反応条件

後処理

1. 1
   温度by heating at 45° for 4 hour

実験手順

Essentially the technique for the appropriate intermediate of Example 22 was used, but substituting 3-(t-butoxycarbonylamino)pyridazine (293 mg, 1.5 mM) for the pyrazine analogue. The reaction was carried out by heating at 45° for 4 hour, and the chromatography was carried out with a gradient from 0% to 100% ethyl acetate in dichloromethane. Relevant fractions were combined to give the desired product (315 mg).

出典