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Dichloromethane → (2R)-8-Fluoro-2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl 4-methylbenzenesulfonate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Dichloromethane | HCID 6344 | — |
| 反応物 | o-Toluenesulfonyl chloride | HCID 8623 | — |
| 反応物 | [(2S)-8-Fluoro-2,3-dihydro-1,4-benzodioxin-2-YL]methanol | HCID 54461939 | — |
| 触媒 | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| 生成物 | (2R)-8-Fluoro-2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl 4-methylbenzenesulfonate | HCID 10759436 | — |
反応手順
Preparation according to Preparation 22 using [(2S)-8-fluoro-2,3-dihydro-1,4-benzodioxin-2-yl]methanol (7.05 g, 38.0 mmol), toluenesulfonyl chloride (10.9 g, 57 mmol), TEA (8.0 ml, 57 mmol) and 4-DMAP (4.7 g, 38.0 mmol) in DCM (75 ml), stirred for 1.5 h. Flash column chromatography yielded 11.9 g of the title compound. MS m/z (rel. intensity, 70 eV) 184 (90), 153 (43), 139 (29), 128 (bp), 57 (25).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08524766B2 |
| 出典データセット | uspto-grants-2013_09 |
| ORD ID | ord-dc7db1bed65a49a697f7dc2bacc6624c |
| 出典メモ | uspto-grants-2013_09 |