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頁籤選單縮合
題名 | A Very Simple Synthesis of 4-(N,N-Dimethylamino)phenol=氰中毒解毒劑DMAP新穎製備法 |
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作者 | 李安榮; 黃文鑫; 王大鵬; 張立乾; 李震東; | 書刊名 | 醫學研究 |
卷期 | 15:6 1995.05[民84.05] |
頁次 | 頁417-428 |
分類號 | 418.82 |
關鍵詞 | 4-N,N-二甲胺酚; 氰中毒; 解毒劑; 合成; 軍陣藥學; 4-(N,N-Dimethylamino)phenol; DMAP; Cyanide poisoning; Antidote; Synthesis; Military pharmancy; |
語文 | 英文(English) |
中文摘要 | 本研究首次發現氰中毒解毒劑DMAP之極簡易合成法。DMAP解毒迅速,療效確實,且副作用少,為最優良之氰中毒解毒劑。本品並無市售,必需自行合成。文獻製備法步驟繁雜,產率過低,且純化費時,不具生產價值。本實驗巧妙設計DMAP之新穎製備法,利用反應起始物對甲氧苯胺(p-anisidine)之甲氧基,其中性及安定性使酚基不致干擾反應,但仍保有強釋電子活性,對甲氧苯胺與過量之磷酸甲酯反應,所得中間產品濃縮物直接水解、洗滌,即得產物DMAP,總產率達87%(文獻法5-10%)。本發明之特點為合成方法簡單,條件溫和,試藥便宜,不需高溫故可避免使用高準點溶媒,不需分離純化中間產品,不需使用減壓分餾裝置,故極易量產,深具軍陣藥學價值。 |
英文摘要 | 4-(N, N-Dimethylamino) phenol (DMAP) (1) is one of the most potent and reliable antidotes for the treatment of acute cyanide poisoning. It exhibits a rapid onset time and does not show significant adverse effects in humans. The mechanism of action and pharmacokinetics of DMAP have been well studied. However, DMAP is not commercially available. Our laboratories have established a very simple, efficient synthesis, suitable for the scale-up pilot-plant preparation, for the preparation of DMAP by reaction of p-anisidine with excessive trimethyl phosphate followed by treatment with 47% hydrobromic acid. The merits of this elegant approach are simple, inexpensive and under mild conditions, which made it extremely attractive for application in the field of synthetic military pharmacy. |
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