반응식
I[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][C:3]=1[OH:8].B1(B2OC(C)(C)C(C)(C)O2)OC(C)(C)C(C)(C)O1.C([O-])(=O)C.[K+].Br[C:33]1[NH:34][C:35]2[CH:36]=[CH:37][CH:38]=[C:39]3[C:45](=[O:46])[NH:44][CH2:43][CH2:42][C:41]=1[C:40]=23.C(=O)([O-])[O-].[Na+].[Na+]>C1C=CC(P(C2C=CC=CC=2)[C-]2C=CC=C2)=CC=1.C1C=CC(P(C2C=CC=CC=2)[C-]2C=CC=C2)=CC=1.Cl[Pd]Cl.[Fe+2]>[OH:8][C:3]1[CH:4]=[CH:5][CH:6]=[CH:7][C:2]=1[C:33]1[NH:34][C:35]2[CH:36]=[CH:37][CH:38]=[C:39]3[C:45](=[O:46])[NH:44][CH2:43][CH2:42][C:41]=1[C:40]=23참가 물질
반응물 5
생성물 1
시약·촉매·용매 1
실험 절차
In a manner similar to that described for Example YY, 2-iodophenol (220 mg, 1.00 mmol), diboron pinacol ester (279 mg, 1.10 mmol), 1,1′-bis(diphenyl phosphino)ferrocenedichloro palladium (24 mg, 0.03 mmol), and potassium acetate (294 mg, 3.00 mmol), 2-bromo-3,4,5,6-tetrahydro-azepino[5,4,3-cd]indol-6-one (239 mg, 0.90 mmol), a second portion of 1,1′-bis(diphenylphosphino)ferrocene dichloropalladium (24 mg, 0.03 mmol), and sodium carbonate (2.5 mL of a 2.0 M aqueous solution, 5.00 mmol) were reacted to yield 2-(2-hydroxy-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one, 40 mg (15%) as a white solid: m.p. 305° C. (dec); 1H NMR (300 MHz, d6-DMSO) δ 2.86 (m, 2H), 3.46 (m, 2H), 6.92 (t, J=7.5 Hz, 1H), 7.00 (d, J=7.8 Hz, 1H), 7.16 (t, J=7.8 Hz, 1H), 7.24 (m, 1H), 7.34 (dd, J=7.5, 1.2 Hz, 1H), 7.55 (d, J=7.8 Hz, 1H), 7.66 (d, J=7.5 Hz, 1H), 8.00 (br t, 1H), 9.84 (br s, 1H), 11.20 (br s, 1H). MS (FAB, MH+): 279. Anal. (C17H14N2O2.0.44 CHCl3) C, H, N.
출처 및 근거
- ORD 기록
- ord-95a3b00ccdb54398b888ffa14faf45f6
- 출처 데이터셋
- uspto-grants-2005_12
- 특허 번호
- US06977298B2
연결된 노트
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