tert-Butyl 4-(4-(7-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)thieno[3,2-b]pyridine-2-yl)phenyl)piperazine-1-carboxylate → N-(3-Fluoro-4-(2-(4-(piperazin-1-yl)phenyl)thieno[3,2-b]pyridin-7-yloxy)phenylcarbamothioyl)-2-phenylacetamide di-hydrochloride
反応式
[ClH:1].FC1C=C(NC(NC(=O)CC2C=CC=CC=2)=S)C=CC=1OC1C=CN=C2C=C(C(NC[C@H]3CCNC3)=O)SC=12.[F:41][C:42]1[CH:76]=[C:75]([NH:77][C:78]([NH:80][C:81](=[O:89])[CH2:82][C:83]2[CH:88]=[CH:87][CH:86]=[CH:85][CH:84]=2)=[S:79])[CH:74]=[CH:73][C:43]=1[O:44][C:45]1[CH:50]=[CH:49][N:48]=[C:47]2[CH:51]=[C:52]([C:54]3[CH:59]=[CH:58][C:57]([N:60]4[CH2:65][CH2:64][N:63](C(OC(C)(C)C)=O)[CH2:62][CH2:61]4)=[CH:56][CH:55]=3)[S:53][C:46]=12>>[ClH:1].[ClH:1].[F:41][C:42]1[CH:76]=[C:75]([NH:77][C:78]([NH:80][C:81](=[O:89])[CH2:82][C:83]2[CH:84]=[CH:85][CH:86]=[CH:87][CH:88]=2)=[S:79])[CH:74]=[CH:73][C:43]=1[O:44][C:45]1[CH:50]=[CH:49][N:48]=[C:47]2[CH:51]=[C:52]([C:54]3[CH:55]=[CH:56][C:57]([N:60]4[CH2:65][CH2:64][NH:63][CH2:62][CH2:61]4)=[CH:58][CH:59]=3)[S:53][C:46]=12参加物
3
反応物 2
生成物 1
実験手順
Following the procedure described above for the synthesis of compound 137a (scheme 25, example 97) but substituting compound 135b for the compound 158, title compound 159 was obtained in 21% yield. 1H NMR (400 MHz, DMSO-d6) δ ppm: 12.48(s, 1H), 11.84(s, 1H), 9.26(bs, 1H), 8.62(d, J=5.6 Hz, 1H), 8.05(d, J=12.0 Hz, 1H), 7.94(s, 1H), 7.81(d, J=8.8 Hz, 2H), 7.62-7.55(m, 2H), 7.37-7.31(m, 4H), 7.31-7.24(m, 1H), 7.10(d, J=8.8 Hz, 2H), 6.85(d, J=5.6 Hz, 1H), 3.83(s, 2H), 3.58-3.51(m, 4H), 3.26-3.18(m, 4H). LRMS (M+1) 597.2 (100%).
出典と根拠
- ORDレコード
- ord-a224aa205fb245049d4f0fbb4a145ee7
- 出典データセット
- uspto-grants-2010_08
- 特許番号
- US07772247B2
反応ノート
読み込み中…