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HRID 79304作成日:2026年10月25日
Cesium carbonate → (S)-tert-butyl 3-(6-((3-ethyl-4-(imidazo[1,2-a]pyridine-3-carboxamido)-1H-indazol-1-yl)methyl)pyridin-2-yloxy)pyrrolidine-1-carboxylate
https://huagongshe.com/reaction/79304
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | Tert-butyl (3R)-3-(methanesulfonyloxy)pyrrolidine-1-carboxylate | HCID 10934372 | — |
| 反応物 | HCID 178437935 | HCID 178437935 | — |
| 溶媒 | Dimethylacetamide | HCID 31374 | — |
| 生成物 | (S)-tert-butyl 3-(6-((3-ethyl-4-(imidazo[1,2-a]pyridine-3-carboxamido)-1H-indazol-1-yl)methyl)pyridin-2-yloxy)pyrrolidine-1-carboxylate | HCID 70814880 | 50.6% |
反応手順
To N-(3-ethyl-1-((6-hydroxypyridin-2-yl)methyl)-1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide (21 mg, 0.051 mmol) in DMA (2 mL) was added (R)-tert-butyl 3-(methylsulfonyloxy)pyrrolidine-1-carboxylate (20 mg, 0.076 mmol) and Cs2CO3 (33 mg, 0.10 mmol). The reaction vial was sealed, and the reaction was heated to 90° C. and stirred for 6 hours. DMA was removed under reduce pressure. The residue was diluted with EtOAc (20 mL), washed with saturated NaHCO3 aqueous solution (5 mL) and brine (5 mL), and concentrated. Silica gel chromatography of the crude material (DCM/MeOH 10:0.5) provided the desired product (15 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08841455B2 |
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| 出典データセット | uspto-grants-2014_09 |
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| ORD ID | ord-1885a0e738a94714aea0ffd29319f71a |
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| 出典メモ | uspto-grants-2014_09 |
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