| 第 36 卷第 1 期 |  | Vol. 36 No. 1 | | 2006 年 2 月 | Feb 2006 |
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所屬欄目：醫藥及中間體
HIV病毒抑制劑中間體5-戊基間苯二酚的合成 |
| 徐宇倫; 張龍; 金鑫; 宋義新(長(cháng)春工業(yè)大學(xué)化工學(xué)院; 大連兆科生化有限公司; 吉林長(cháng)春; 遼寧大連) |
| 摘 要：以3,5-二甲氧基苯甲酸為起始原料,與LiH在室溫下反應5h生成苯甲酸鹽,生成的鹽再與正丁基鋰進(jìn)行�；磻玫�3,5-二甲氧基苯戊酮,進(jìn)而在210℃以下進(jìn)行烏爾夫-黃鳴龍反應將酮還原,生成3,5-二甲氧基戊苯,所得產(chǎn)物與吡啶鹽酸鹽熔融,于200℃回流2h,脫甲基制得5-戊基間苯二酚,總收率達60.9%,純度≥98%。 |
| 關(guān)鍵詞：3; 5-二甲氧基苯甲酸; �；�; 烏爾夫-黃鳴龍還原; 5-戊基間苯二酚 |
| 中圖分類(lèi)號：TQ243.1 文獻標識碼：A 文章編號：1009-9212(2006)01-0027-03 |
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| Synthesis of HIV Inhibitor Intermediate 5-Pentyl Resorcinol |
| XU Yu-lun1; ZHANG Long1; JIN Xin2; SONG Yi-xin2（1.School of Chemical and Engineering; Changchun University of Technology; Changchun 130012; China; 2.Dalian Zhaoke Biochemical Co.; Ltd; Dalian 116620; China） |
| Abstract：3,5-Dimethoxybenzoic acid reacts with lithium hydride to form salt which is acylated by n-butyllithium to synthesize 1-(3,5-dimethoxyphenyl)-1-pentanone,and then this ketone is reduced by Wolff L-Huangminglong reaction under 210 ℃ to form 3,5-dimethoxy-1-phenylbenzene that refluxs with pyridine and concentrated hydrochloric acid for 2 h at 200 ℃ to prepare 5-pentyl resorcinol.The total yield of 5-pentyl resorcinol is up to 60.9% and its purity is no less than 98%. |
| Key words：3; 5-dimethoxybenzoic acid; acylation; Wolff L-Huangminglong reaction; 5-pentyl resorcinol |
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收稿日期：2005-09-11
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