関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | (2R)-2-aminopentan-1-ol | HCID 5324727 | — |
| 反応物 | 2-Bromo-4-(4-bromo-phenyl)-thiazole | HCID 68538161 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | HCID 86618495 | HCID 86618495 | 83% |
反応手順
A mixture of 2-bromo-4-(4-bromophenyl)-1,3-thiazole (2.9 g, 9.09 mmol), prepared in step 2 of Example 1, and (R)-(−)-2-amino-pentanol (2.82 g, 27.2 mmol) was stirred under nitrogen at 150° C. for 18 h. After cooling to room temperature, the residue was taken up in methylene chloride, applied to a Biotage FLASH 40+™ cartridge and the methylene chloride allowed to evaporate. Purification of the residue on the samplet on a Horizon™ Flash Collector (the Biotage FLASH 40+™ cartridge) using a linear gradient of 5% ethyl acetate-hexane to 100% ethyl acetate gave (2R)-2-{[4-(4-bromophenyl)-1,3-thiazol-2-yl]amino}pentan-1-ol (2.56 g, 83%) as a yellow solid, mp 63-65° C.; MS (ESI) m/z 341 [M+H]+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07538107B2 |
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| 出典データセット | uspto-grants-2009_05 |
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| ORD ID | ord-f6b4c6a0d5ca41188558e370445d8d8c |
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| 出典メモ | uspto-grants-2009_05 |
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