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1H-Benzotriazole-1-carboxaldehyde → (S)-N-[[3-[3-Fluoro-4-[1-(formyl)-3-azetidinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1H-Benzotriazole-1-carboxaldehyde | HCID 576740 | — |
| 反応物 | (S)-N-[[3-[3-Fluoro-4-[3-azetidinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide | HCID 53667482 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | (S)-N-[[3-[3-Fluoro-4-[1-(formyl)-3-azetidinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide | HCID 54095930 | — |
反応手順
N-Formylbenzotriazole (115 mg, 0.78 mmol) was added to a stirred suspension of (S)-N-[[3-[3-fluoro-4-[3-azetidinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide (Example 82, 153 mg, 0.50 mmol) in THF (5 mL) and stirred overnight. The solvent was removed and the residue chromatographed over silica gel (50 g, 40-60 μm) eluting with 2-5% methanol-chloroform to give the title compound as a white foam. FAB-HRMS: theory 336.1356 (M+1); meas. 336.1357.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06166056 |
| 出典データセット | uspto-grants-2000_12 |
| ORD ID | ord-789d1dfcb93e45bea7a4e97c9025381f |
| 出典メモ | uspto-grants-2000_12 |