(1R,2S)-1-[(5-bromo-3,6-diethylpyrazin-2-yl)amino]-2,3-dihydro-1H-inden-2-ol → methyl (3R,4S)-3-[(5-bromo-3,6-diethylpyrazin-2-yl)amino]-4-(2-fluoroethoxy)pyrrolidine-1-carboxylate
반응식
[Br:1]C1N=C(CC)C(N[C@@H]2C3C(=CC=CC=3)C[C@@H]2O)=NC=1CC.[CH2:23]([C:25]1[C:26]([NH:33][C@H:34]2[C@@H:38]([O:39][CH2:40][CH2:41][F:42])[CH2:37][N:36]([C:43]([O:45][CH3:46])=[O:44])[CH2:35]2)=[N:27][C:28]([CH2:31][CH3:32])=[CH:29][N:30]=1)[CH3:24]>>[Br:1][C:29]1[N:30]=[C:25]([CH2:23][CH3:24])[C:26]([NH:33][C@H:34]2[C@@H:38]([O:39][CH2:40][CH2:41][F:42])[CH2:37][N:36]([C:43]([O:45][CH3:46])=[O:44])[CH2:35]2)=[N:27][C:28]=1[CH2:31][CH3:32]참가 물질
3
반응물 2
생성물 1
실험 절차
Following the procedure for the preparation of (1R,2S)-1-[(5-bromo-3,6-diethylpyrazin-2-yl)amino]-2,3-dihydro-1H-inden-2-ol but substituting methyl(3R,4S)-3-[(3,6-diethylpyrazin-2-yl)amino]-4-(2-fluoroethoxy)pyrrolidine-1-carboxylate and making non-critical variations provided the title compound as a oil: 1H NMR (400 MHz, DMSO-d6) δ) 6.12, 4.49, 4.37, 4.21, 3.69–3.39, 2.71–2.55, 1.20–1.12; IR (liq.) 2973 (s), 2957, 2068 (b), 1996, 1705 (s), 1561 (s), 1541 (s), 1481 (s), 1454 (s), 1392 (s), 1191 (s), 1175, 1140 (s), 1114 (s), 1048, cm−1; HRMS (FAB) calcd for C16H24BrFN4O3+H 419.1094, found 419.1112. Anal. Calcd for C16H24BrFN4O3: C, 45.83; H, 5.77; N, 13.36. Found: C, 45.49; H, 5.81; N, 13.03.