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5-(Hydroxymethyl)-1H-benzimidazole → [1-(6-{[1-(4-fluorophenyl)ethyl]amino}pyrazin-2-yl)-1H-benzimidazol-6-yl]methanol
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 5-(Hydroxymethyl)-1H-benzimidazole | HCID 13505556 | — |
| 反応物 | 6-chloro-N-[1-(4-fluorophenyl)ethyl]pyrazin-2-amine | HCID 54940806 | — |
| 生成物 | [1-(6-{[1-(4-fluorophenyl)ethyl]amino}pyrazin-2-yl)-1H-benzimidazol-6-yl]methanol | HCID 11337446 | 8.1% |
反応手順
In a procedure analogous to Example 3, reaction of 6-chloro-N-[1-(4-fluorophenyl)ethyl]pyrazin-2-amine (1.80 g, 7.15 mmol) and 5-hydroxymethyl benzimidazole (1.26 g, 8.5 mmol) furnished the two products which were separated by column chromatography using dichloromethane-methanol (98:2-92:8) as eluant. From the less polar fractions was obtained [1-(6-{[1-(4-fluorophenyl)ethyl]amino}pyrazin-2-yl)-1H-benzimidazol-6-yl]methanol as a pale yellow solid (210 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07737143B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-4cc787ad7b6243cfaee5cf52752f4bfd |
| 出典メモ | uspto-grants-2010_06 |