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HRID 974870作成日:2026年10月25日
Pyridine → O-benzhydryl (6R)-3-(1,3-benzoxazol-2-yl)-7-[[(2Z)-2-methoxyimino-2-[2-(tritylamino)-1,3-thiazol-4-yl]acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carbothioate
https://huagongshe.com/reaction/974870
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
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| 反応物 | Pyridine | HCID 1049 | — |
| 反応物 | Phosphorus oxychloride | HCID 24813 | — |
| 反応物 | (Z)-2-methoxymino-2-(2-(tritylamino)thiazol-4-yl)acetic acid | HCID 5928144 | — |
| 反応物 | Diphenylmethyl 7-amino-3-(benzoxazol-2-yl)thio-3-cephem-4-carboxylate | HCID 131719875 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | O-benzhydryl (6R)-3-(1,3-benzoxazol-2-yl)-7-[[(2Z)-2-methoxyimino-2-[2-(tritylamino)-1,3-thiazol-4-yl]acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carbothioate | HCID 172974451 | 72% |
反応手順
A 207 mg portion of diphenylmethyl 7-amino-3-(benzoxazol-2-yl)thio-3-cephem-4-carboxylate was dissolved in 4 ml of methylene chloride and the resulting solution was cooled to -20° C. To this were added 213 mg of (Z)-2-(2-tritylaminothiazol-4-yl)-2-methoxyiminoaceticacid, 0.13 ml of pyridine and 45 μl of phosphorous oxychloride, followed by 20 minutes of stirring at the same temperature. The resulting solution was mixed with 4 ml of water, stirred for additional 1 hour at room temperature, and then subjected to organic layer separation. After drying the resulting organic layer on anhydrous magnesium sulfate and distilling off the solvent under a reduced pressure, the residue was purified by a column chromatography (30 g silica gel, toluene:ethyl acetate =3:1) to obtain 272 mg of the title compound (yield, 72%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US05607927 |
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| 出典データセット | uspto-grants-1997_03 |
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| ORD ID | ord-f3e6386fd9e244d0bfa587380522b92f |
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| 出典メモ | uspto-grants-1997_03 |
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