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Triethylamine → Methyl 3-(4-{1-[6-(4-trifluoromethyl-phenyl)-pyridin-3-yl]-heptyloxy}-benzoylamino)-propionoate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide | HCID 15908 | — |
| 反応物 | Methyl beta-alanate | HCID 192794 | — |
| 反応物 | 4-{1-[6-(4-Trifluoromethyl-phenyl)-pyridin-3-yl]-heptyloxy}-benzoic acid | HCID 67342206 | — |
| 触媒 | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | Methyl 3-(4-{1-[6-(4-trifluoromethyl-phenyl)-pyridin-3-yl]-heptyloxy}-benzoylamino)-propionoate | HCID 67153427 | 95.8% |
反応手順
To a mixture of 4-{1-[6-(4-trifluoromethyl-phenyl)-pyridin-3-yl]-heptyloxy}-benzoic acid (230 mg, 0.5 mmol) in methylene chloride (5 mL) are added triethyl amine (0.21 mL, 1.51 mmol), DMAP (5.0 mg), 3-amino-propionic acid methyl ester (210.5 mg, 1.51 mmol) and EDCI (290 mg, 1.51 mmol) at room temperature. The reaction mixture is stirred at room temperature overnight, loaded on silica gel, eluted with eluted with hexanes with a gradient from 0% of ethyl acetate to 100% of ethyl acetate giving methyl 3-(4-{1-[6-(4-trifluoromethyl-phenyl)-pyridin-3-yl]-heptyloxy}-benzoylamino)-propionoate (260 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07989457B2 |
| 出典データセット | uspto-grants-2011_08 |
| ORD ID | ord-b5815f1b83e840e19459e773cfb9fa20 |
| 出典メモ | uspto-grants-2011_08 |