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Methanol → (2s)-(-)-1-(4-Indolyloxy)-3-(4-hydroxy-4-(3-trifluoromethylphenyl)piperidin-1-yl)-2-propanol ethanedioate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Methanol | HCID 887 | — |
| 反応物 | Oxalic Acid | HCID 971 | — |
| 反応物 | 4-[3-(Trifluoromethyl)phenyl]-4-piperidinol | HCID 75255 | — |
| 反応物 | (2s)-Glycidyl indol-4-yl ether | HCID 10943254 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | (2s)-(-)-1-(4-Indolyloxy)-3-(4-hydroxy-4-(3-trifluoromethylphenyl)piperidin-1-yl)-2-propanol ethanedioate | HCID 131719677 | — |
反応手順
The title compound was prepared in similar fashion from (S)-(+)-4-(oxiranylmethoxy)-1H-indole and 4-hydroxy-4-(3-trifluoromethylphenyl)piperidine. The resulting free base was dissolved in ethyl acetate, and precipitated with one equivalent of oxalic acid in ethyl acetate in 59% overall yield. FDMS m/e=426 (M+ of free base). α[D]589 =-11.39 (c=0.56, methanol).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05789402 |
| 出典データセット | uspto-grants-1998_08 |
| ORD ID | ord-f772bd01abad40f8a0b1b0b3554d9ce6 |
| 出典メモ | uspto-grants-1998_08 |