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O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate → 6-[4-(7-Methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-5-methyl-pyrimidine-4-carboxylic acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate | HCID 2733207 | — |
| 反応物 | 5-Fluoroindoline | HCID 2774463 | — |
| 反応物 | Tert. butyl 6-[4-(7-methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-5-methyl-pyrimidin-4-carboxylate | HCID 58386534 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 6-[4-(7-Methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-5-methyl-pyrimidine-4-carboxylic acid | HCID 58386435 | — |
反応手順
70 mg (0.17 mmol) tert. butyl 6-[4-(7-methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-5-methyl-pyrimidin-4-carboxylate, 26 mg (0.19 mmol) 5-fluoroindoline, 61 mg (0.19 mmol) TBTU and 27 μL (0.19 mmol) TEA were stirred in 1.0 mL DMF for 3 h at RT. The reaction mixture was purified by HPLC. The product-containing fractions were combined and freeze-dried.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08829006B2 |
| 出典データセット | uspto-grants-2014_09 |
| ORD ID | ord-a503c57dd4264e0c8f32ab98bd540b0c |
| 出典メモ | uspto-grants-2014_09 |