2,2,2-Trifluoroethyl trifluoromethanesulfonate → [5-[3-(3-Aza-bicyclo[3.1.0]hex-3-yl)-propoxy]-1-(2,2,2-trifluoro-ethyl)-1H-indol-2-yl]-morpholin-4-yl-methanone

HRID 132827

반응식

HRID 132827 반응식
[OH:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[N:7]([CH2:11][C:12]([F:15])([F:14])[F:13])[C:6]([C:16]([N:18]1[CH2:23][CH2:22][O:21][CH2:20][CH2:19]1)=[O:17])=[CH:5]2.[CH:24]12[CH2:29][CH:28]1[CH2:27][N:26]([CH2:30][CH2:31][CH2:32]OC1C=C3C(=CC=1)NC(C(N1CCOCC1)=O)=C3)[CH2:25]2.FC(F)(F)COS(C(F)(F)F)(=O)=O>>[CH:24]12[CH2:29][CH:28]1[CH2:27][N:26]([CH2:30][CH2:31][CH2:32][O:1][C:2]1[CH:3]=[C:4]3[C:8](=[CH:9][CH:10]=1)[N:7]([CH2:11][C:12]([F:15])([F:13])[F:14])[C:6]([C:16]([N:18]1[CH2:23][CH2:22][O:21][CH2:20][CH2:19]1)=[O:17])=[CH:5]3)[CH2:25]2

참가 물질

4

반응물 3

HCID 803662,2,2-Trifluoroethyl trifluoromethanesulfonateHCID 16754253{5-[3-(3-Aza-bicyclo[3.1.0]hex-3-yl)-propoxy]-1H-indol-2-yl}-morpholin-4-yl-methanoneHCID 67527268[5-Hydroxy-1-(2,2,2-trifluoro-ethyl)-1H-indol-2-yl]-morpholin-4-yl-methanone

생성물 1

HCID 16112804[5-[3-(3-Aza-bicyclo[3.1.0]hex-3-yl)-propoxy]-1-(2,2,2-trifluoro-ethyl)-1H-indol-2-yl]-morpholin-4-yl-methanone

실험 절차

In analogy to the procedure described for the synthesis of intermediate 1, step 1, the title compound was synthesized from {5-[3-(3-aza-bicyclo[3.1.0]hex-3-yl)-propoxy]-1H-indol-2-yl}-morpholin-4-yl-methanone (Example 5, step 4) and 2,2,2-trifluoroethyl-trifluoromethanesulfonate. The title product was obtained in 45% yield as white solid. MS (m/e): 452.5 (MH+, 100%).

출처 및 근거

ORD 기록
ord-e70956c355d04fa79af0aaa0a047a06f
출처 데이터셋
uspto-grants-2008_06
특허 번호
US07388095B2

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