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Triphenylphosphine → 6-[2-(1,1-dioxothiomorpholin-4-yl)ethoxy]-3-(3,5-difluorophenyl)-2-(pyridin-3-yl)-1H-inden-1-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triphenylphosphine | HCID 11776 | — |
| 反応物 | Diisopropyl azodicarboxylate | HCID 5363146 | — |
| 反応物 | 4-(2-Hydroxyethyl)-1lambda~6~,4-thiazinane-1,1-dione | HCID 21874811 | — |
| 反応物 | 2-bromo-6-hydroxy-3-phenyl-1H-inden-1-one | HCID 70306176 | — |
| 反応物 | 3-(3,5-difluorophenyl)-6-hydroxy-2-(pyridin-3-yl)-1H-inden-1-one | HCID 70317432 | — |
| 生成物 | 6-[2-(1,1-dioxothiomorpholin-4-yl)ethoxy]-3-(3,5-difluorophenyl)-2-(pyridin-3-yl)-1H-inden-1-one | HCID 51002042 | — |
反応手順
The procedure of Step 6 of Example 1 was repeated except for using 3-(3,5-difluorophenyl)-6-hydroxy-2-(pyridin-3-yl)-1H-inden-1-one obtained in Step 1 of Example 64 as a starting material instead of 2-bromo-6-hydroxy-3-phenyl-1H-inden-1-one, 4-(2-hydroxyethyl)thiomorpholine-1,1-dioxide (2.0 eq) instead of 4-(2-hydroxyethyl)morpholine, using 2 equivalents of PPh3 and DIAD, and being stirred for 13 h to provide 6-[2-(1,1-dioxothiomorpholin-4-yl)ethoxy]-3-(3,5-difluorophenyl)-2-(pyridin-3-yl)-1H-inden-1-one, which was treated with HCl/dioxane following the same procedure in Step 8 of Example 1 (40% for 2 steps).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08877747B2 |
| 出典データセット | uspto-grants-2014_11 |
| ORD ID | ord-29c45d38f96b47feb9884b78f171a199 |
| 出典メモ | uspto-grants-2014_11 |