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Bis(2-oxo-3-oxazolidinyl)phosphinic chloride → 1H-Benzoimidazole-2-carboxylic acid (1-pyrimidin-4-yl-piperidin-4-yl)-amide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Bis(2-oxo-3-oxazolidinyl)phosphinic chloride | HCID 152842 | — |
| 反応物 | 2-Benzimidazolecarboxylic acid | HCID 233240 | — |
| 反応物 | Sodium Bicarbonate | HCID 516892 | — |
| 反応物 | 1-Pyrimidin-4-yl-piperidin-4-ylamine trifluoroacetate | HCID 22394384 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Triethylamine | HCID 8471 | — |
| 生成物 | 1H-Benzoimidazole-2-carboxylic acid (1-pyrimidin-4-yl-piperidin-4-yl)-amide | HCID 86009867 | — |
反応手順
To a solution of 80 mg 1H-Benzoimidazole-2-carboxylic acid in 1 mL DMF and 0.2 mL NEt3, 200 mg 1-Pyrimidin-4-yl-piperidin-4-ylamine trifluoroacetate and 125 mg BOP-Cl were added and the mixture was stirred for 3 h. Finally, 3 mL saturated NaHCO3 solution were added and the mixture was filtered through a chem elut® cartridge by elution with ethyl acetate. After removal of the solvent under reduced pressure the crude product was subjected to the next reaction step without further purification. Yield: 160 mg.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07741341B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-79f71b05143e49688872fd3f6a5d773c |
| 出典メモ | uspto-grants-2010_06 |