Serinol → 2-(1,3-Dihydroxyprop-2-ylamino)-8-isopropyl-4-[4-(pyridin-2-yl)benzylamino]pyrazolo[1,5-a]-1,3,5-triazine
反応式
[OH:1][CH2:2][C@H:3]([NH:6][C:7]1[N:12]=[C:11]([NH:13][CH2:14][C:15]2[CH:20]=[CH:19][C:18]([C:21]3[CH:26]=[CH:25][CH:24]=[CH:23][N:22]=3)=[CH:17][CH:16]=2)[N:10]2[N:27]=[CH:28][C:29]([CH:30]([CH3:32])[CH3:31])=[C:9]2[N:8]=1)[CH2:4]C.NC(CO)C[OH:36]>>[OH:36][CH2:4][CH:3]([NH:6][C:7]1[N:12]=[C:11]([NH:13][CH2:14][C:15]2[CH:16]=[CH:17][C:18]([C:21]3[CH:26]=[CH:25][CH:24]=[CH:23][N:22]=3)=[CH:19][CH:20]=2)[N:10]2[N:27]=[CH:28][C:29]([CH:30]([CH3:31])[CH3:32])=[C:9]2[N:8]=1)[CH2:2][OH:1]参加物
3
実験手順
According to the same conditions resulting in the preparation of the compound 2, the compound 17 is prepared from IIa.2 by oxidation reaction of the sulfur atom and then introduction of serinol. Yield=30%. Oil. 1H NMR (300 MHz, CDCl2): δ 8.68 (d, 1H, J=4.4 Hz, Harom), 7.96 (d, 2H, J=8.3 Hz, Harom), 7.79-7.69 (m, 2H, Harom) 7.64 (s, 1H, Harom) 7.45 (d, 2H, J=8.3 Hz, Harom) 7.26-7.21 (m, 1H, Harom), 6.80 (bs, 1H, NH), 5.71 (bs, 1H, NH), 4.77 (d, 2H, J=5.9 Hz, CH2), 4.08-4.95 (m, 1H, CH), 3.92-3.80 (m, 4H, 2 CH2), 3.02 (hept, 1H, J=7.0 Hz, CH), 1.28 (d, 6H, J=7.0 Hz, 2 CH3). MS (ESI): m/z 434 (MH+).