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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
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | N,N,N',N'-Tetramethylazodicarboxamide | HCID 4278 | — |
| 反応物 | Tributylphosphine | HCID 13831 | — |
| 反応物 | [Rac]-2-(6-hydroxy-indol-1-yl)-propionic acid ethyl ester | HCID 68826438 | — |
| 反応物 | [2-(2,2,2-trifluoro-ethyl)-5-(4-trifluoromethoxy-phenyl)-2H-pyrazol-3-yl]-methanol | HCID 86600629 | — |
| 生成物 | [Rac]-2-{6-[2-(2,2,2-trifluoro-ethyl)-5-(4-trifluoromethoxy-phenyl)-2h-pyrazol-3-ylmethoxy]-indol-1-yl}-propionic acid ethyl ester | HCID 87766039 | — |
反応手順
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.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07265149B2 |
| 出典データセット | uspto-grants-2007_09 |
| ORD ID | ord-230b193bda9f441e977a1b73d3156c68 |
| 出典メモ | uspto-grants-2007_09 |