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HRID 2053530作成日：2026年10月25日
3,5-Difluorobenzylamine → tert-butyl (4S,5R)-2-[(3,5-difluorophenyl)methylamino]-4,5-diphenyl-4,5-dihydroimidazole-1-carboxylate
https://huagongshe.com/reaction/2053530
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 3,5-Difluorobenzylamine | HCID 145211 | — |
| 反応物 | cis-4,5-Diphenyl-2-methylthio-4,5-dihydro-imidazole-1-carboxylic Acid, Tert-Butyl Ester | HCID 86596320 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 生成物 | tert-butyl (4S,5R)-2-[(3,5-difluorophenyl)methylamino]-4,5-diphenyl-4,5-dihydroimidazole-1-carboxylate | HCID 68569310 | 44.4% |
反応手順
A mixture of intermediate 59 (0.50 g, 1.36 mmol), 3,5-difluorobenzylamine (0.481 mL, 4.07 mmol) and MeOH (0.1 mL) is heated at 100° C. for 3 days. The reaction mixture is cooled to RT, and is purified by chromatography on silica gel; gradient elution with heptane:EtOAc (75:25-60:40) gives 0.28 g of the product 89. 1H NMR (CDCl3) δ 7.10-6.60 (m, 14H), 5.45-5.35 (m, 2H), 4.75-4.55 (m, 2H), 1.16 (s, 9H); MS: m/z 464 (M++1).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07326792B2 |
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| 出典データセット | uspto-grants-2008_02 |
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| ORD ID | ord-4a854ebd720842dc9e87b1dde0f63483 |
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| 出典メモ | uspto-grants-2008_02 |
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