| 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
三光氣法合成降糖藥格列美脲 |
| 劉占科; 楊新武; 盧其慧; 王曉光; 劉智凌(湖南海利化工股份有限公司; 珠海三鑫精細化工有限公司; 湖南化工研究院; 湖南長(cháng)沙; 廣東珠海) |
| 摘 要：2-苯乙胺、反式-4-甲基環(huán)己胺分別與三光氣反應生成相應的異氰酸酯。2-苯乙基異氰酸酯與3-乙基-4-甲基-3-吡咯啉-2-酮加成(收率87.2%)后,經(jīng)磺化、氨解(收率78.1%)得到的取代磺酰胺,再與反式-4-甲基環(huán)己基異氰酸酯反應得到格列美脲,收率75.1%。標題化合物總收率51.1%(以吡咯啉酮計),含量99.6%(反式)。 |
| 關(guān)鍵詞：三光氣; 光氣; 2-苯乙基異氰酸酯; 反式-4-甲基環(huán)己基異氰酸酯; 格列美脲; 降糖藥 |
| 中圖分類(lèi)號：R977.1+5 文獻標識碼：A 文章編號：1009-9212(2006)03-0016-03 |
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| Synthesis of Antidiabetic Glimepiride with Triphosgene |
| LIU Zhan-ke1; YANG Xin-wu1; LU Qi-hui2; WANG Xiao-guang1; 3; LIU Zhi-ling3（1.Hunan Haili Chemical Industry Co.; Ltd.; Changsha 410007; China; 2.Zhuhai Sanxin Fine Chemical Co.; Zhuhai 519041; 3.Hunan Research Institute of Chemical Industry; China） |
| Abstract：β-phenylethyl isocyanate and tran-1-isocyanato-4-methyl cyclohexane were prepared through reaction of β-phenylethylamine and trans-4-methyl clyclohexanamine with triphosgene,respectively.Addition of β-phenylethylisocyanate and 3-ethyl-4-methyl-pyrrolin-2-one to yield intermediate substituted sulfamide via sulfonation and amination,and then the substituted sulfamide was reacted with trans-1-isocyanato-4-methylcyelohexane to yield glimepiride with its overall yield and purity is of 51.1% and 99.6%,respectivel... |
| Key words：triphosgene; phosgene; 2-phenylethyl isocyanate; trans-1-isocyanato-4-methyl cyclohexane; glimepiride; antidiabetic |
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收稿日期：2005-12-18
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