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(RS)-N,N-dimethyl-{2-[4-(alpha-phenyl-p-chloro-benzyl)piperazin-1-yl]ethoxy}-acetamide → Cetirizine Hydrochloride
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | (RS)-N,N-dimethyl-{2-[4-(alpha-phenyl-p-chloro-benzyl)piperazin-1-yl]ethoxy}-acetamide | HCID 10180126 | — |
| 反応物 | (RS)-N,N-diethyl-{2-[4-(alpha-phenyl-p-chloro-benzyl)piperazin-1-yl]ethoxy}-acetamide | HCID 22391920 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | Cetirizine Hydrochloride | HCID 55182 | 74.9% |
反応手順
The procedure described in Example 14 is followed with the difference that, instead of the (RS)-N,N-dimethyl-{2-[4-(α-phenyl-p-chloro-benzyl)piperazin-1-yl]ethoxy}-acetamide, 104.4 g (0.2 moles) of (RS)-N,N-diethyl-{2-[4-(α-phenyl-p-chloro-benzyl)piperazin-1-yl]ethoxy}-acetamide are used, 100 ml of dioxane are employed as cosolvent, and, during the alkaline hydrolysis, the reaction mixture is boiled for 4 hours. Thus, 69.1 g (74.9%) of the title compound are obtained, m.p.: 225-228° C. The purity of the product corresponds to the quality requirements given in Eur. Pharm., 3, 1997, 1084.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06908999B2 |
| 出典データセット | uspto-grants-2005_06 |
| ORD ID | ord-daf8c77284af4de28b716c7be08bfd2d |
| 出典メモ | uspto-grants-2005_06 |