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

HRID 278007

반응식

HRID 278007 반응식
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

참가 물질

3

반응물 2

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

생성물 1

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

실험 절차

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.

출처 및 근거

ORD 기록
ord-5c2a057212ee49f6aef2d3e848561246
출처 데이터셋
uspto-grants-2002_03
특허 번호
US06358972B1

연결된 노트

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