化工社化工社 化学情報印刷レポート · 研究参考用
HRID 15333作成日：2026年10月27日
8-Bromo-2,3-dihydro-1,4-benzodioxine-6-carbaldehyde → Racemic methyl 2-[3-fluoro-6-(methyloxy)-1,5-naphthyridin-4-yl]-3-[(cis)-3-fluoro-4-({[(phenylmethyl)oxy]carbonyl}amino)-1-piperidinyl]propanoate
https://huagongshe.com/reaction/15333
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 8-Bromo-2,3-dihydro-1,4-benzodioxine-6-carbaldehyde | HCID 16637176 | — |
| 反応物 | Furo[2,3-c]pyridin-5-ylmethanol | HCID 22047174 | — |
| 反応物 | Methyl 2-[3-fluoro-6-(methyloxy)-1,5-naphthyridin-4-yl]-2-propenoate | HCID 57486873 | — |
| 反応物 | benzyl N-[(3R,4S)-3-fluoropiperidin-4-yl]carbamate | HCID 68566554 | — |
| 触媒 | 1,1,3,3-Tetramethylguanidine | HCID 66460 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | Racemic methyl 2-[3-fluoro-6-(methyloxy)-1,5-naphthyridin-4-yl]-3-[(cis)-3-fluoro-4-({[(phenylmethyl)oxy]carbonyl}amino)-1-piperidinyl]propanoate | HCID 68685415 | 100% |
反応手順
A solution of methyl 2-[3-fluoro-6-(methyloxy)-1,5-naphthyridin-4-yl]-2-propenoate (953 mg, 3.63 mmol), cis-phenylmethyl[3-fluoro-4-piperidinyl]carbamate Enantiomer 2 (for a synthesis see WO2004058144, prepared by analogy to Examples 142(b), (c) and (d) from the Enantiomer 2 of Example 142(a)) (1.1 g, 4.35 mmol) and 1,1,3,3-tetramethylguanidine (6 drops) in DMF (3.5 ml) was heated at 80° C. under argon for 3 hours, cooled and evaporated. Chromatography, eluting with 1% methanol/dichloromethane, gave the product in 100% yield.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07732461B2 |
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| 出典データセット | uspto-grants-2010_06 |
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| ORD ID | ord-721d8cceaacc48fea2c0ccf5e6db4a4c |
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| 出典メモ | uspto-grants-2010_06 |
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