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Diisopropylethylamine → (S)-tert-butyl 3-(2-chloro-5-fluoropyrimidin-4-ylamino)pyrrolidine-1-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | 2,4-Dichloro-5-fluoropyrimidine | HCID 250705 | — |
| 反応物 | tert-butyl (3S)-3-aminopyrrolidine-1-carboxylate | HCID 854071 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | (S)-tert-butyl 3-(2-chloro-5-fluoropyrimidin-4-ylamino)pyrrolidine-1-carboxylate | HCID 86667413 | 102.7% |
反応手順
To a mixture of 2,4-dichloro-5-fluoro-pyrimidine (1.75 g, 10.48 mmol) and iPr2NEt (3.27 mL, 18.78 mmol) in THF (50 mL) was added tert-butyl (3S)-3-aminopyrrolidine-1-carboxylate (1.83 mL, 10.48 mmol) in THF (2 mL). The resulting solution was allowed to stir at room temperature for 2 hours. The mixture was concentrated to dryness, diluted with dichloromethane and washed with water. The organic layer was dried over Na2SO4 and concentrated in vacuo to afford 3.41 g of 7a, as a white foamy solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09345708B2 |
| 出典データセット | uspto-grants-2016_05 |
| ORD ID | ord-3e75715202f3455289ef3294b0c6a79b |
| 出典メモ | uspto-grants-2016_05 |