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HRID 279664作成日：2026年10月26日
Triphenylphosphine → 7-(2-(Imidazol-1-yl)ethoxy)-6-methoxy-3-((pivaloyloxy)methyl)-3,4-dihydroquinazolin-4-one
https://huagongshe.com/reaction/279664
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Triphenylphosphine | HCID 11776 | — |
| 反応物 | N-(2-Hydroxyethyl)imidazole | HCID 74168 | — |
| 反応物 | ethyl N-ethoxycarbonyliminocarbamate | HCID 220568 | — |
| 反応物 | (7-Hydroxy-6-methoxy-4-oxoquinazolin-3(4H)-yl)methyl pivalate | HCID 10804576 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 7-(2-(Imidazol-1-yl)ethoxy)-6-methoxy-3-((pivaloyloxy)methyl)-3,4-dihydroquinazolin-4-one | HCID 22030782 | 80% |
反応手順
Diethyl azodicarboxylate (435 mg, 2.5 mmol) was added dropwise to a suspension of 7-hydroxy-6-methoxy-3-((pivaloyloxy)methyl)-3,4-dihydroquinazolin-4-one (612 mg, 2 mmol), (prepared as described for the starting material in Example 85), 2-(imidazol-1-yl)ethanol (280 mg, 2.5 mmol), (J. Med. Chem. 1993, 25 4052-4060), and triphenylphosphine (655 mg, 2.5 mmol) in methylene chloride (10 ml) at 5° C. The mixture was stirred for 10 minutes at 5° C. and then 1 hour at ambient temperature. The mixture was poured directly on to a silica column and eluted with methylene chloride/methanol (95/5) to give 7-(2-(imidazol-1-yl)ethoxy)-6-methoxy-3-((pivaloyloxy)methyl)-3,4-dihydroquinazolin-4-one (640 mg, 80%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US06362336B1 |
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| 出典データセット | uspto-grants-2002_03 |
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| ORD ID | ord-d9c62763225047ae9a0430a506c014f0 |
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| 出典メモ | uspto-grants-2002_03 |
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