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HRID 1177637作成日：2026年10月27日
Acetic Acid → (3R)-3-(tert-butoxycarbonylamino)-4-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl)phenylamino)-4-oxobutanoic acid
https://huagongshe.com/reaction/1177637
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Acetic Acid | HCID 176 | — |
| 反応物 | 3-Fluoro-4-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl)benzenamine | HCID 57403052 | — |
| 反応物 | (R)-tert-butyl 2,5-dioxo-tetrahydrofuran-3-ylcarbamate | HCID 86597499 | — |
| 溶媒 | Benzene | HCID 241 | — |
| 生成物 | (3R)-3-(tert-butoxycarbonylamino)-4-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl)phenylamino)-4-oxobutanoic acid | HCID 67111578 | — |
反応手順
To 3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl)benzenamine (206 mg, 0.570 mmol) and (R)-tert-butyl 2,5-dioxo-tetrahydrofuran-3-ylcarbamate (123 mg, 0.570 mmol) was added benzene (5.7 mL) and acetic acid (163 μl, 2.85 mmol) before it was stirred at 80° C. for 1 h. The two regioisomers were separated via SFC (Column: Princeton Pyridine, Mobile Phase: 60:40 liquid CO2/MeOH) to give (3R)-3-(tert-butoxycarbonylamino)-4-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl)phenylamino)-4-oxobutanoic acid and its regioisomer. MS (ESI) m/z: Calculated: 576.2; Observed: 577.1 (M++H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07842685B2 |
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| 出典データセット | uspto-grants-2010_11 |
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| ORD ID | ord-819a09bc986e43bebea2680b06368edb |
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| 出典メモ | uspto-grants-2010_11 |
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