関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Hydrochloric Acid | HCID 313 | — |
| 反応物 | Erlotinib | HCID 176870 | — |
| 溶媒 | Isopropanol | HCID 3776 | — |
| 生成物 | Erlotinib Hydrochloride | HCID 176871 | 91.5% |
反応手順
Into a 1 Lt. four necked round-bottomed flask provided with a mechanical stirrer, thermometer socket, reflux condenser etc., are charged 325 mL of isopropyl alcohol, followed by 25.0 g of Erlotinib base (Prepared according to the process given in Example-(1) of PCT International Publication No. WO 2007/060691) at 70-75° C. so that Erlotinib base completely dissolves in the solvent. Then carbon treatment is given and the filtrate is transferred to another 1 Lt. four-necked round bottomed flask provided with all the necessary accessories. To this solution isoproponolic HCl (HCl content as 100% is 2.548 g) is added in one lot at 60-65° C. and maintained at this temperature for about 1 hour. The reaction mass is cooled to room temperature and filtered. The product is washed with fresh isopropyl alcohol and dried to get 25.0 g of Erlotinib hydrochloride as a white crystalline powder.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08748602B2 |
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| 出典データセット | uspto-grants-2014_06 |
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| ORD ID | ord-69683049ff534bd4896aaa11134eeab0 |
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| 出典メモ | uspto-grants-2014_06 |
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