第 36 卷第 3 期 |  | Vol. 36 No. 3 | 2006 年 6 月 | Jun 2006 |
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所屬欄目:醫藥及中間體
赤式-2-(2,4-二氟苯基)-3-甲基-2-[(1H-1,2,4-三唑-1-基)甲基]環(huán)氧乙烷的合成 |
黃漢忠; 李樹(shù)軍(天津藥物研究院化學(xué)制藥研究部) |
摘 要:以間二氟苯為原料,經(jīng)傅克;、水解、環(huán)合等反應制得三唑丁醇類(lèi)抗真菌藥物的重要中間體赤式-2-(2,4-二氟苯基)-3-甲基-2-[(1H-1,2,4-三唑-1-基)甲基]環(huán)氧乙烷,總收率44.6%,純度98%以上(HPLC),工藝穩定,利于工業(yè)生產(chǎn)。 |
關(guān)鍵詞:赤式-2-(2; 4-二氟苯基)-3-甲基-2-[(1H-1; 2; 4-三唑-1-基)甲基]環(huán)氧乙烷; 化學(xué)合成; 工藝研究; 抗真菌藥 |
中圖分類(lèi)號:TQ223.2+6 文獻標識碼:A 文章編號:1009-9212(2006)03-0014-02 |
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Synthesis of Erythro-2-(2,4-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)methyl]Oxirane |
HUANG Han-zhong; LI Shu-jun(Tianjin Institute of Pharmaceutical Research; Tianjin 300193; China) |
Abstract:Erythro-2-(2,4-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)methyl] oxirane(1)is a key intermediate of antifungal triazolybutanol compounds.Title compound(1) was synthesized from 1,3-difluorobenzene via Friedel-crafts,hydrolysis,cyclization,etc.The total yield and purity is 44.6% and 98%,respectively. |
Key words:erythro-2-(2; 4-difluorophenyl)-3-methyl-2-[(1H-1; 2; 4-triazol-1-yl)methyl] oxirane; Chemical synthesis; process research; antifungal triazolybutanol compounds |
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收稿日期:2006-03-10
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