N,N,N',N'-Tetramethylazodicarboxamide → [Rac]-2-{6-[2-(2,2,2-trifluoro-ethyl)-5-(4-trifluoromethoxy-phenyl)-2h-pyrazol-3-ylmethoxy]-indol-1-yl}-propionic acid ethyl ester

HRID 915480

반응식

HRID 915480 반응식
[CH2:1]([O:3][C:4](=[O:17])[CH:5]([N:7]1[C:15]2[C:10](=[CH:11][CH:12]=[C:13]([OH:16])[CH:14]=2)[CH:9]=[CH:8]1)[CH3:6])[CH3:2].[F:18][C:19]([F:40])([F:39])[CH2:20][N:21]1[C:25]([CH2:26]O)=[CH:24][C:23]([C:28]2[CH:33]=[CH:32][C:31]([O:34][C:35]([F:38])([F:37])[F:36])=[CH:30][CH:29]=2)=[N:22]1.CN(C)C(N=NC(N(C)C)=O)=O.C(P(CCCC)CCCC)CCC>>[CH2:1]([O:3][C:4](=[O:17])[CH:5]([N:7]1[C:15]2[C:10](=[CH:11][CH:12]=[C:13]([O:16][CH2:26][C:25]3[N:21]([CH2:20][C:19]([F:39])([F:18])[F:40])[N:22]=[C:23]([C:28]4[CH:33]=[CH:32][C:31]([O:34][C:35]([F:37])([F:38])[F:36])=[CH:30][CH:29]=4)[CH:24]=3)[CH:14]=2)[CH:9]=[CH:8]1)[CH3:6])[CH3:2]

참가 물질

5

반응물 4

HCID 4278N,N,N',N'-TetramethylazodicarboxamideHCID 13831TributylphosphineHCID 68826438[Rac]-2-(6-hydroxy-indol-1-yl)-propionic acid ethyl esterHCID 86600629[2-(2,2,2-trifluoro-ethyl)-5-(4-trifluoromethoxy-phenyl)-2H-pyrazol-3-yl]-methanol

생성물 1

HCID 87766039[Rac]-2-{6-[2-(2,2,2-trifluoro-ethyl)-5-(4-trifluoromethoxy-phenyl)-2h-pyrazol-3-ylmethoxy]-indol-1-yl}-propionic acid ethyl ester

실험 절차

In analogy to the procedure described for example 3 c], [rac]-2-(6-hydroxy-indol-1-yl)-propionic acid ethyl ester (J. E. D. Barton, D. Cartwright, C. J. Mathews, Brit. UK Pat. Appl. (1992), GB 2253848 A1) was reacted with [2-(2,2,2-trifluoro-ethyl)-5-(4-trifluoromethoxy-phenyl)-2H-pyrazol-3-yl]-methanol (example 15 b]) in the presence of N,N,N′,N′-tetramethyl azodicarboxamide and tributylphosphine to give [rac]-2-{6-[2-(2,2,2-trifluoro-ethyl)-5-(4-trifluoromethoxy-phenyl)-2H-pyrazol-3-ylmethoxy]-indol-1-yl}-propionic acid ethyl ester as colorless oil.

출처 및 근거

ORD 기록
ord-230b193bda9f441e977a1b73d3156c68
출처 데이터셋
uspto-grants-2007_09
특허 번호
US07265149B2

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