반응 #70478

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Methanesulfonic acid 2-[4-(4-benzyl-phthalazin-1-yl)-3,4,5,6-tetrahydro-2H-[1,2′]bipyrazinyl-5′-yl]-2-hydroxy-propyl ester

4-hydroxy piperidine

diisoproylethylamine

→

title compound

수율 24.1%

1-{2-[4-(4-Benzyl-phthalazin-1-yl)-3,4,5,6-tetrahydro-2H-[1,2′]bipyrazinyl-5′-yl]-2-hydroxy-propyl}-piperidin-4-ol

수율 24.1%

용매

acetonitrile

반응 조건

후처리

1. 1
   온도The mixture is heated
2. 2
   온도to reflux for 16 h
3. 3
   농축Concentrate the crude mixture in vacuo
4. 4
   기타The residue is purified by flash chromatography on silica gel (MeOH/CH2Cl2)

실험 절차

Methanesulfonic acid 2-[4-(4-benzyl-phthalazin-1-yl)-3,4,5,6-tetrahydro-2H-[1,2′]bipyrazinyl-5′-yl]-2-hydroxy-propyl ester (64 mg, 0.120 mmol) is combined with 4-hydroxy piperidine (61 mg, 0.600 mmol), diisoproylethylamine (63 μL, 0.360 mmol), and acetonitrile (1 mL). The mixture is heated to reflux for 16 h. Concentrate the crude mixture in vacuo. The residue is purified by flash chromatography on silica gel (MeOH/CH2Cl2) to afford the title compound (15.6 mg, 24%).

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