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1-Aminotetralin, (S)- → 1-{6[(1S)-1,2,3,4-tetrahydronaphthalen-1-ylamino]pyrazin-2-yl}-1H-benzimidazole-6-carbonitrile
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1-Aminotetralin, (S)- | HCID 7058074 | — |
| 反応物 | 1-(6-chloropyrazin-2-yl)-1H-benzimidazole-6-carbonitrile | HCID 11345856 | — |
| 反応物 | 1-(6-chloropyrazin-2-yl)-1H-benzimidazole-5-carbonitrile | HCID 58869934 | — |
| 生成物 | 1-{6[(1S)-1,2,3,4-tetrahydronaphthalen-1-ylamino]pyrazin-2-yl}-1H-benzimidazole-6-carbonitrile | HCID 11187710 | — |
反応手順
In an analogous fashion to Example 1, an approximately 1:1 mixture of 1-(6-chloropyrazin-2-yl)-1H-benzimidazole-5-carbonitrile and 1-(6-chloropyrazin-2-yl)-1H-benzimidazole-6-carbonitrile (100 mg, 0.39 mmol) was condensed with (1S)-1,2,3,4-tetrahydronaphthalen-1-amine (69 mg, 0.47 mmol). The product was obtained as a mixture of regioisomers which were separated by column chromatography using dichloromethane-methanol (95:5) as eluant. From the less polar fractions 1-{6[(1S)-1,2,3,4-tetrahydronaphthalen-1-ylamino]pyrazin-2-yl}-1H-benzimidazole-6-carbonitrile was obtained as a yellow semi-solid (26 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-df8b0ec0c5c04a37b7ab3bd35f278c0e |
| 出典メモ | uspto-grants-2010_06 |