3,5-Bis-trifluoromethylphenylboronic acid → 5-(3,5-Di(trifluoromethyl)phenyl)-3-(1-Methylpiperidin-4-yl)-4-Aza-1H-Indole

HRID 278007ノート

反応式

HRID 278007 の反応式
FC(F)(F)S(O[C:7]1[N:8]=[C:9]2[C:13](=[CH:14][CH:15]=1)[NH:12][CH:11]=[C:10]2[CH:16]1[CH2:21][CH2:20][N:19]([CH3:22])[CH2:18][CH2:17]1)(=O)=O.[F:25][C:26]([F:41])([F:40])[C:27]1[CH:28]=[C:29](B(O)O)[CH:30]=[C:31]([C:33]([F:36])([F:35])[F:34])[CH:32]=1>>[F:25][C:26]([F:40])([F:41])[C:27]1[CH:28]=[C:29]([C:7]2[N:8]=[C:9]3[C:13](=[CH:14][CH:15]=2)[NH:12][CH:11]=[C:10]3[CH:16]2[CH2:17][CH2:18][N:19]([CH3:22])[CH2:20][CH2:21]2)[CH:30]=[C:31]([C:33]([F:34])([F:35])[F:36])[CH:32]=1

参加物

3

反応物 2

HCID 1562653,5-Bis-trifluoromethylphenylboronic acidHCID 120418125-Trifluoromethanesulfonyloxy-3-(1-methylpiperidin-4-yl)pyrrolo[3,2-b]pyridine

生成物 1

HCID 98671915-(3,5-Di(trifluoromethyl)phenyl)-3-(1-Methylpiperidin-4-yl)-4-Aza-1H-Indole収率 90.7%

実験手順

O-Trifluoromethanesulfonyl-3-(1-methylpiperidin-4-yl)-5-hydroxy-4-aza-1H-indole (160 mg, 0.441 mmol) and 3,5-di(trifluoromethyl)phenylboronic acid (183 mg, 0.71 mmol) were converted to 171 mg of the title compound by the procedure of Example 3. (91%). MS(FD) m/e 427.6 (M+). EA calculated for C21H19F6N3: C, 59.02; H, 4.45; N, 9.84. Found: C, 59.31; H, 4.69; N, 9.83.

出典と根拠

ORDレコード
ord-5c2a057212ee49f6aef2d3e848561246
出典データセット
uspto-grants-2002_03
特許番号
US06358972B1

反応ノート

読み込み中…