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Diisopropylethylamine → (S)-1-[6-Cyclopropylmethoxy-5-(3,3-difluoro-azetidin-1-yl)-pyridine-2-carbonyl]-4,4-difluoro-pyrrolidine-2-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 | O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate | HCID 2733207 | — |
| 反応物 | 4,4-Difluoro-L-prolinamide hydrochloride | HCID 45158909 | — |
| 反応物 | 6-(Cyclopropylmethoxy)-5-(3,3-difluoroazetidin-1-yl)picolinic acid | HCID 71087292 | — |
| 生成物 | (S)-1-[6-Cyclopropylmethoxy-5-(3,3-difluoro-azetidin-1-yl)-pyridine-2-carbonyl]-4,4-difluoro-pyrrolidine-2-carboxylic acid amide | HCID 118451458 | — |
反応手順
In analogy to the procedure described in Example 47 b), 6-cyclopropylmethoxy-5-(3,3-difluoro-azetidin-1-yl)-pyridine-2-carboxylic acid (Example 1 b)) was reacted with (S)-4,4-difluoropyrrolidine-2-carboxamide hydrochloride (426844-51-1) in the presence of TBTU and DIEA to obtain the title compound as colorless oil; MS (EI): m/e=417.5 [MH+].
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09303012B2 |
| 出典データセット | uspto-grants-2016_04 |
| ORD ID | ord-b23b46c9475f4e8785205698a3855173 |
| 出典メモ | uspto-grants-2016_04 |