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1,4-Dioxane → (S)-1-(1-{4-[3-(4-Ethoxy-phenoxy)-azetidin-1-yl]-phenyl}-ethyl)-3-pyrimidin-4-yl-urea
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1,4-Dioxane | HCID 31275 | — |
| 反応物 | 4-Aminopyrimidine | HCID 68958 | — |
| 反応物 | 1,8-Diazabicyclo(5.4.0)undec-7-ene | HCID 81184 | — |
| 反応物 | (S)-1-{4-[3-(4-Ethoxy-phenoxy)-azetidin-1-yl]-phenyl}-ethylamine | HCID 86689010 | — |
| 生成物 | (S)-1-(1-{4-[3-(4-Ethoxy-phenoxy)-azetidin-1-yl]-phenyl}-ethyl)-3-pyrimidin-4-yl-urea | HCID 71616306 | — |
反応手順
0.03 mL (0.20 mmol) DBU and 0.033 g (0.20 mmol) CDT are added to 0.010 g (0.10 mmol) 4-aminopyrimidine in 1.0 mL 1,4-dioxane. The mixture is stirred for 5 min at rt followed by addition of 0.048 g (0.092 mmol) (S)-1-{4-[3-(4-ethoxy-phenoxy)-azetidin-1-yl]-phenyl}-ethylamine (X.1) in 1.0 mL 1,4-dioxane. The mixture is stirred for 12 h at rt and subsequently concentrated in vacuo. The residue is purified by HPLC (XBridge, ACN/water (+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-30a23b06abe14314b3991ac4d9ca0352 |
| 出典メモ | uspto-grants-2013_09 |