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1-Cyclopropyl-1-(5-methyl-1,2,4-oxadiazol-3-yl)ethan-1-amine → 5-Cyclopropyl-4-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-pyridine-2-carboxylic acid [1-cyclopropyl-1-(5-methyl-[1,2,4]oxadiazol-3-yl)-ethyl]-amide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1-Cyclopropyl-1-(5-methyl-1,2,4-oxadiazol-3-yl)ethan-1-amine | HCID 43559223 | — |
| 反応物 | 5-Cyclopropyl-4-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-pyridine-2-carboxylic acid | HCID 90204573 | — |
| 生成物 | 5-Cyclopropyl-4-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-pyridine-2-carboxylic acid [1-cyclopropyl-1-(5-methyl-[1,2,4]oxadiazol-3-yl)-ethyl]-amide | HCID 74763822 | — |
反応手順
The mixture of epimers was synthesized in analogy to Example 63b, using 5-Cyclopropyl-4-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-pyridine-2-carboxylic acid (Example 68a) and 1-Cyclopropyl-1-(5-methyl-[1,2,4]oxadiazol-3-yl)-ethylamine (CAN 1155536-64-3) as starting materials and isolated (135 mg, 58%) as a light yellow oil. The mixture of epimers was separated into its epimers by preparative chiral HPLC (Chiralpak AD, ethanol/heptane) and the title compound was the first epimer collected and isolated as colorless oil; MS (ESI, m/z): 425.5 (M+H+).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09409866B2 |
| 出典データセット | uspto-grants-2016_08 |
| ORD ID | ord-9f5cf8f5488242eda0e56fe2de91689e |
| 出典メモ | uspto-grants-2016_08 |