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HRID 237869作成日:2026年10月25日
Ethyl 3-cyclopropylprop-2-ynoate → (S)-2-(4-Bicyclo[3.3.1]non-9-yl-phenoxymethyl)-5-cyclopropyl-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-one
https://huagongshe.com/reaction/237869
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Ethyl 3-cyclopropylprop-2-ynoate | HCID 639964 | — |
| 反応物 | (S)-5-(4-bicyclo[3.3.1]non-9-yl-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine | HCID 68527534 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 生成物 | (S)-2-(4-Bicyclo[3.3.1]non-9-yl-phenoxymethyl)-5-cyclopropyl-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-one | HCID 25070149 | 16% |
反応手順
To a solution of (S)-5-(4-bicyclo[3.3.1]non-9-yl-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine (0.7 g, 2.23 mmol) (Example 20) in ethanol (40 mL) was added 0.462 g (3.35 mmol) of cyclopropyl-propynoic acid ethyl ester (Example 99). The reaction mixture was stirred at 82° C. for 30 minutes. The reaction mixture was concentrated and purified by chromatography on silica gel, eluting with MeOH/CH2Cl2 to afford 0.145 g of the title compound. [α]D25 −10.51 (c 0.5, CHCl3).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08642603B2 |
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| 出典データセット | uspto-grants-2014_02 |
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| ORD ID | ord-494112d35e844939b647719951059f8e |
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| 出典メモ | uspto-grants-2014_02 |
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