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Diisopropylethylamine → 1-[2-[3-(3,4-Dichloro-phenyl)-1-(3,4,5-trifluoro-benzoyl)-pyrrolidin-3-yl]-ethyl]-4-phenyl-piperidine-4-carboxylic acid amide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | 3,4,5-Trifluorobenzoic acid | HCID 853154 | — |
| 反応物 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 反応物 | 1-Hydroxybenzotriazole hydrate | HCID 2796029 | — |
| 反応物 | 2-(3-(3,4-Dichlorophenyl)pyrrolidin-3-yl)ethanol | HCID 18464427 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 1-[2-[3-(3,4-Dichloro-phenyl)-1-(3,4,5-trifluoro-benzoyl)-pyrrolidin-3-yl]-ethyl]-4-phenyl-piperidine-4-carboxylic acid amide | HCID 54496518 | — |
反応手順
Combine 3-(3,4-dichloro-phenyl)-3-(2-hydroxyethyl)-pyrrolidine (286 mg, 1.1 mmol), 3,4,5-trifluoro-benzoic acid (1 mmol), N,N-diisopropylethylamine (0.19 mL, 1.1 mmol), 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) (0.21 g, 1.1 mmol), and 1-hydroxybenzotriazole hydrate (HOBT) (0.15 g, 1.1 mmol) in dichloromethane (10 mL). After 18 hour, dilute with dichloromethane and extract with 1M hydrochloric acid solution, 5% sodium bicarbonate solution, and water. Dry the organic layer over MgSO4, filter, and evaporate in vacuo to give the title compound: Rf =0.45 (silica gel, 10% methanol/dichloromethane).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05861416 |
| 出典データセット | uspto-grants-1999_01 |
| ORD ID | ord-a0313b695a6d40229de23cea780efbb5 |
| 出典メモ | uspto-grants-1999_01 |