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Losartan → Losartan potassium salt
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Losartan | HCID 3961 | — |
| 反応物 | Potassium Hydroxide | HCID 14797 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | Isopropanol | HCID 3776 | — |
| 溶媒 | Heptane | HCID 8900 | — |
| 生成物 | Losartan potassium salt | HCID 11476710 | 77.1% |
反応手順
As already described, to 10.2 g crude losartan of Example 14 (chromatographic purity 98.73%) in 59 ml i-propanol, a solution of 1.4 g potassium hydroxide in 1.5 ml water at a temperature of 38-40° C. to a pH of 10 over half an hour was added. Approximately 19 ml of azeotropic mixture i-propanol/water were removed by distillation, 36 ml n-heptane were added, and reaction mixture was stirred at room temperature until a white solid was formed. The resulting mixture was diluted with 14 ml n-heptane, filtered, washed with 26 ml n-heptane, and dried in vacuo at 50° C. to yield 8.57 g losartan potassium (yield: 77%, chromatographic purity: 99.67%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07271269B2 |
| 出典データセット | uspto-grants-2007_09 |
| ORD ID | ord-90f75912b30741d4915d400fd59d5da6 |
| 出典メモ | uspto-grants-2007_09 |