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Diisopropylethylamine → [6-Cyclopropylmethoxy-5-(3,3-difluoro-azetidin-1-yl)-pyridin-2-yl]-(6-oxa-1-aza-spiro[3.3]hept-1-yl)-methanone
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 | 6-(Cyclopropylmethoxy)-5-(3,3-difluoroazetidin-1-yl)picolinic acid | HCID 71087292 | — |
| 反応物 | 6-Oxa-1-azaspiro[3.3]heptane oxalate | HCID 71303992 | — |
| 生成物 | [6-Cyclopropylmethoxy-5-(3,3-difluoro-azetidin-1-yl)-pyridin-2-yl]-(6-oxa-1-aza-spiro[3.3]hept-1-yl)-methanone | HCID 76281875 | — |
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 6-oxa-1-azaspiro[3.3]heptane oxalate (CAN 1359655-43-8) in the presence of TBTU and DIEA to give the title compound as colorless oil; MS (EI): m/e=366.4 [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-44d5d39a5cd64879b63d4cb2fd51f04d |
| 出典メモ | uspto-grants-2016_04 |