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Water → (S)-N-(1-{4-[3-(2-Morpholin-4-yl-pyrimidin-4-yloxy)-azetidin-1-yl]-phenyl}-ethyl)-acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | Sodium hydride | HCID 24758 | — |
| 反応物 | 4-(4-Chloropyrimidin-2-yl)morpholine | HCID 824643 | — |
| 反応物 | (S)-N-{1-[4-(3-Hydroxy-azetidin-1-yl)-phenyl]ethyl}-acetamide | HCID 86689005 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | (S)-N-(1-{4-[3-(2-Morpholin-4-yl-pyrimidin-4-yloxy)-azetidin-1-yl]-phenyl}-ethyl)-acetamide | HCID 86689029 | — |
反応手順
To 30 mg (0.15 mmol) 4-(4-chloro-pyrimidin-2-yl)-morpholine in DMF (1.0 mL) is added 30 mg (0.13 mmol) (S)—N-{1-[4-(3-hydroxy-azetidin-1-yl)-phenyl]-ethyl}-acetamide (V.1) in DMF (1.0 mL). 20 mg (0.45 mmol, 55% in mineral oil) NaH is added and the mixture is stirred for 12 h at room temperature. Water is added, the mixture is concentrated in vacuo and the residue is purified by HPLC (XBridge, acetronitrile/H2O (+0.1% NH4OH)) to yield the desired product.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08530461B2 |
| 出典データセット | uspto-grants-2013_09 |
| ORD ID | ord-2cb6b7a8d71d4622a531371718e86c94 |
| 出典メモ | uspto-grants-2013_09 |