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HRID 56374作成日：2026年10月25日
1,8-Diazabicyclo(5.4.0)undec-7-ene → tert-butyl ((1S,2R)-2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)cyclohexyl)carbamate
https://huagongshe.com/reaction/56374
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 1,8-Diazabicyclo(5.4.0)undec-7-ene | HCID 81184 | — |
| 反応物 | (1S,2R)-Cyclohexane-1,2-diamine, N1-BOC protected | HCID 1514389 | — |
| 反応物 | 2-Chloro-6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazoline | HCID 89921772 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | tert-butyl ((1S,2R)-2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)cyclohexyl)carbamate | HCID 118043439 | 81% |
反応手順
A mixture of 2-chloro-6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazoline (0.95 g, 2.6 mmol), tert-butyl ((1S,2R)-2-aminocyclohexyl)carbamate (1.1 g, 5.14 mmol), and DBU (0.77 mL, 5.14 mmol) in acetonitrile (9 mL) was degassed with N2 for 5 mins and heated at 70° C. for 16 h. The mixture was cooled to room temperature, concentrated and the residue was purified by silica gel column chromatography to afford tert-butyl ((1S,2R)-2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)cyclohexyl)carbamate (1.1 g, 81%). MS (ES+) C27H32Cl2N4O4 requires: 546, found: 547 [M+H]+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US09434700B2 |
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| 出典データセット | uspto-grants-2016_09 |
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| ORD ID | ord-69a23d5d36bf4cc69ee11cb718be1394 |
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| 出典メモ | uspto-grants-2016_09 |
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