Ethanolamine → HCID 72709697、化合物
反応式
Cl[C:2]1[N:7]=[CH:6][C:5]([C:8](=[O:32])[CH2:9][N:10]2[C:15]3=[N:16][C:17]([N:21]4[CH2:26][C@@H:25]5[CH2:27][C@H:22]4[CH2:23][O:24]5)=[CH:18][C:19](=[O:20])[N:14]3[CH2:13][CH2:12][C@H:11]2[C:28]([F:31])([F:30])[F:29])=[CH:4][CH:3]=1.[CH2:33]([CH2:35][NH2:36])[OH:34]>C(O)C>[OH:34][CH2:33][CH2:35][NH:36][C:2]1[N:7]=[CH:6][C:5]([C:8](=[O:32])[CH2:9][N:10]2[C:15]3=[N:16][C:17]([N:21]4[CH2:26][C@@H:25]5[CH2:27][C@H:22]4[CH2:23][O:24]5)=[CH:18][C:19](=[O:20])[N:14]3[CH2:13][CH2:12][C@H:11]2[C:28]([F:31])([F:30])[F:29])=[CH:4][CH:3]=1参加物
4
反応条件
- 温度
- 130 °C
実験手順
A mixture of 0.50 mL of ethanol, 33 mg (0.070 mmol) of (8S)-9-[2-(6-chloropyrid-3-yl)-2-oxoethyl]-2-(1S,4S)-2-oxa-5-azabicyclo[2.2.1]hept-5-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 21.41 μl (0.352 mmol) of ethanolamine is heated in a Biotage microwave reactor at 130° C. for 30 minutes. The reaction mixture is evaporated to dryness and the residue is then taken up in 10 mL of water. The precipitate is filtered off and then dried under vacuum. 17 mg of (8S)-9-{2-[6-(2-hydroxyethylamino)pyrid-3-yl]-2-oxoethyl}-2-(1S,4S)-2-oxa-5-azabicyclo[2.2.1]hept-5-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one are obtained, the characteristics of which are as follows: