反応式
Cl[C:2]1[C:3]2[C:10](I)=[CH:9][N:8]([C@H:12]3[CH2:17][CH2:16][C@H:15]([N:18]4[CH2:23][CH2:22][N:21]([CH3:24])[CH2:20][CH2:19]4)[CH2:14][CH2:13]3)[C:4]=2[N:5]=[CH:6][N:7]=1.[C:25]1([NH:31][C:32](=[O:49])[CH2:33][C:34]2[CH:39]=[CH:38][C:37](B3OC(C)(C)C(C)(C)[O:41]3)=[CH:36][CH:35]=2)[CH:30]=[CH:29][CH:28]=[CH:27][CH:26]=1.CO[C@@H]1[C@@H](C(OC)=O)[C@@H]2[C@@H](C[N:57]3[C@H](C2)C2NC4C=C(OC)C=CC=4C=2CC3)C[C@H]1[O:79][C:80]([C:82]1[CH:87]=[C:86]([O:88]C)C(OC)=C(OC)C=1)=[O:81]>C(#N)C>[C:80]([OH:79])(=[O:81])/[CH:82]=[CH:87]\[C:86]([OH:88])=[O:41].[C:80]([OH:79])(=[O:81])/[CH:82]=[CH:87]\[C:86]([OH:88])=[O:41].[C:80]([OH:79])(=[O:81])/[CH:82]=[CH:87]\[C:86]([OH:88])=[O:41].[C:25]1([NH:31][C:32](=[O:49])[CH2:33][C:34]2[CH:39]=[CH:38][C:37]([C:10]3[C:3]4[C:2]([NH2:57])=[N:7][CH:6]=[N:5][C:4]=4[N:8]([C@H:12]4[CH2:17][CH2:16][C@H:15]([N:18]5[CH2:23][CH2:22][N:21]([CH3:24])[CH2:20][CH2:19]5)[CH2:14][CH2:13]4)[CH:9]=3)=[CH:36][CH:35]=2)[CH:30]=[CH:29][CH:28]=[CH:27][CH:26]=1参加物
5
実験手順
trans-N-phenyl-2-(4-{4-amino-7-[4-(4-methylpiperazino)cyclohexyl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl}phenyl)acetamide trismaleate was prepared from trans-4-chloro-5-iodo-7-[4-(4-methylpiperazino)cyclohexyl]-7H-pyrrolo[2,3-d]pyrimidine (1.0 g, 2.18 mmol) and N1-phenyl -2-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]acetamide in a similar method to that described for the cis-isomer: 1H NMR (DMSO-d6, 400 MHz) 10.18(s, 1H), 8.18(s, 1H), 7.61(d, 2H), 7.51(m, 5H), 7.31(t, 2H), 7.04(t, 1H), 6.3(bs, 2H), 6.11(s, 6H), 4.58(m, 1H), 3.69(s, 2H), 2.6-3.6(bm, 9H), 2.68(s, 3H), 1.91-2.04(m, 6H), 1.51-1.59(m, 2H);); RP-HPLC (Hypersil HS C18, 5 m, 100 A, 250×4.6 mm; 25%-100% acetonitrile over 10 min, 1 mL/min) tr 6.07 min.; MS:MH+ 524.3.
出典と根拠
- ORDレコード
- ord-f13f8b4e6e6f4c5491ff6fee3e3cb166
- 出典データセット
- uspto-grants-2004_03
- 特許番号
- US06713474B2
関連ノート
読み込み中…