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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
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2,2,2-Trifluoroethyl trifluoromethanesulfonate | HCID 80366 | — |
| 反応物 | {5-[3-(3-Aza-bicyclo[3.1.0]hex-3-yl)-propoxy]-1H-indol-2-yl}-morpholin-4-yl-methanone | HCID 16754253 | — |
| 反応物 | [5-Hydroxy-1-(2,2,2-trifluoro-ethyl)-1H-indol-2-yl]-morpholin-4-yl-methanone | HCID 67527268 | — |
| 生成物 | [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 | HCID 16112804 | — |
反応手順
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%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07388095B2 |
| 出典データセット | uspto-grants-2008_06 |
| ORD ID | ord-e70956c355d04fa79af0aaa0a047a06f |
| 出典メモ | uspto-grants-2008_06 |