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Sodium cyanoborohydride → HCID 58852273、化合物
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Sodium cyanoborohydride | HCID 5003444 | — |
| 反応物 | HCID 58852270 | HCID 58852270 | — |
| 反応物 | 6-fluoro-5-methyl-1-piperidin-4-yl-1H-benzoimidazole | HCID 58852309 | — |
| 溶媒 | Acetic Acid | HCID 176 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 生成物 | HCID 58852273 | HCID 58852273 | 24.5% |
反応手順
A mixture of 6-fluoro-5-methyl-1-piperidin-4-yl-1H-benzoimidazole (70 mg, 0.300 mmol) and 5-fluoroindane-2-carbaldehyde (49 mg, 0.300 mmol) in CH3OH (4 mL) and acetic acid (0.2 mL) was stirred at rt for 15 minutes. NaCNBH3 (40 mg, 0.635 mmol) was added and then the reaction mixture was stirred for 1 hour. The solvent was removed and the residue was diluted with CH2Cl2. The organic layers were washed with saturated NaHCO3, brine, and dried over Na2SO4. The organic extracts were removed under the reduced pressure and the residue was purified by flash chromatography (5% CH3OH in CH2Cl2) to afford 6-fluoro-1-[1-(5-fluoro-indan-2-ylmethyl)-piperidin-4-yl]-5-methyl-1H-benzoimidazole (28 mg, 24%) as a white solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07803816B2 |
| 出典データセット | uspto-grants-2010_09 |
| ORD ID | ord-fb4028b2645442c293236945f67d43eb |
| 出典メモ | uspto-grants-2010_09 |