3-Cyanophenylboronic acid → 3-{6-[3-(4-fluorophenyl)-1-trityl-1H-4-pyrazolyl]imidazo[1,2-a]pyridin-3-yl} benzonitrile
反応式
[C:1]([C:3]1[CH:4]=[C:5](B(O)O)[CH:6]=[CH:7][CH:8]=1)#[N:2].[F:12][C:13]1[CH:18]=[CH:17][C:16]([C:19]2[C:23]([C:24]3[CH:25]=[CH:26][C:27]4[N:28]([C:30](I)=[CH:31][N:32]=4)[CH:29]=3)=[CH:22][N:21]([C:34]([C:47]3[CH:52]=[CH:51][CH:50]=[CH:49][CH:48]=3)([C:41]3[CH:46]=[CH:45][CH:44]=[CH:43][CH:42]=3)[C:35]3[CH:40]=[CH:39][CH:38]=[CH:37][CH:36]=3)[N:20]=2)=[CH:15][CH:14]=1>>[F:12][C:13]1[CH:18]=[CH:17][C:16]([C:19]2[C:23]([C:24]3[CH:25]=[CH:26][C:27]4[N:28]([C:30]([C:7]5[CH:8]=[C:3]([CH:4]=[CH:5][CH:6]=5)[C:1]#[N:2])=[CH:31][N:32]=4)[CH:29]=3)=[CH:22][N:21]([C:34]([C:47]3[CH:52]=[CH:51][CH:50]=[CH:49][CH:48]=3)([C:41]3[CH:46]=[CH:45][CH:44]=[CH:43][CH:42]=3)[C:35]3[CH:40]=[CH:39][CH:38]=[CH:37][CH:36]=3)[N:20]=2)=[CH:15][CH:14]=1参加物
3
実験手順
46 mg 3-cyanophenylboronic acid and 161 mg 6-[3-(4-fluorophenyl)-1-trityl-1H-4-pyrazolyl]-3-iodoimidazo[1,2-a]pyridine (compound in Production Example 39) were reacted in the same manner as in Example 3, to give 136 mg 3-{6-[3-(4-fluorophenyl)-1-trityl-1H-4-pyrazolyl]imidazo[1,2-a]pyridin-3-yl} benzonitrile as colorless crystals. This product was subjected to deprotection of the trityl group and converted into the corresponding hydrochloride by the same method as in Example 68, to give 90 mg of the title compound as colorless crystals.
出典と根拠
- ORDレコード
- ord-cd4666a33ca84b58a1bda57659621282
- 出典データセット
- uspto-grants-2006_07
- 特許番号
- US07074801B1
反応ノート
読み込み中…