関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Formic Acid | HCID 284 | — |
| 反応物 | Toluene | HCID 1140 | — |
| 反応物 | Trityl candesartan cilexetil | HCID 11029254 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 生成物 | Candesartan Cilexetil | HCID 2540 | — |
反応手順
Typically, the deprotection step comprises heating to reflux trityl candesartan cilexetil in methanol. Optionally, the deprotection solvent mixture further comprises an organic solvent, such as toluene, and/or an acid, such as formic acid. The cilexetil trityl candesartan is heated to reflux until a clear solution is obtained. Typically, the reaction temperature is from about 30° C. to about 90° C., preferably from about 50° C. to about 90° C., and the heating takes place for about 5 to about 19 hours, preferably for about 8 to about 12 hours. Thereafter, the solvents are removed by evaporation to obtain crude deprotected candesartan cilexetil. The solvents may be removed at a temperature of about 30° C. to about 70° C., preferably at a temperature of about 50° C., and at a reduce pressure of about 30 mbar.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07098342B2 |
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| 出典データセット | uspto-grants-2006_08 |
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| ORD ID | ord-9ddc7e8714f848aa8be681a6021447c6 |
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| 出典メモ | uspto-grants-2006_08 |
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