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HRID 1434585作成日：2026年10月27日
PyBOP → 5-Fluoro-1-methyl-3-{[4-(4-{[3-(1-piperidinyl)propyl]oxy}phenyl)-1-piperazinyl]carbonyl}-1H-indole
https://huagongshe.com/reaction/1434585
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | PyBOP | HCID 2724699 | — |
| 反応物 | 1-[4-(3-Piperidin-1-ylpropoxy)phenyl]piperazine | HCID 9924013 | — |
| 反応物 | 5-fluoro-1-methyl-1H-indole-3-carboxylic acid | HCID 18385102 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 5-Fluoro-1-methyl-3-{[4-(4-{[3-(1-piperidinyl)propyl]oxy}phenyl)-1-piperazinyl]carbonyl}-1H-indole | HCID 57935847 | 15.2% |
反応手順
A solution of 5-fluoro-1-methyl-1H-indole-3-carboxylic acid [WO 0071537 A1] (35 mg) and 1-(4-{[3-(1-piperidinyl)propyl]oxy}phenyl)piperazine (D11) (50 mg) in dichloromethane (1 ml) was treated with benzotriazol-1-yloxytripyrrolidinophosphonium hexafluorophosphate (94.4 mg) and heated in a microwave (CEM™ Discover microwave) at 120° C. for 5 min. The reaction mixture was concentrated in vacuo and purified on a SCX cartridge (2 g) eluting with methanol-aqueous ammonia (10:1) followed by mass directed auto preparative HPLC to give the title compound (12 mg). LCMS RT=2.49 min, 478 (M+H)+
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07615550B2 |
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| 出典データセット | uspto-grants-2009_11 |
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| ORD ID | ord-81824e8f11314bc1a7d9ea2905217a3d |
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| 出典メモ | uspto-grants-2009_11 |
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