| 第 36 卷第 3 期 |  | Vol. 36 No. 3 | | 2006 年 6 月 | Jun 2006 |
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所属栏目：医药及中间体
三光气法合成降糖药格列美脲 |
| 刘占科; 杨新武; 卢其慧; 王晓光; 刘智凌(湖南海利化工股份有限公司; 珠海三鑫精细化工有限公司; 湖南化工研究院; 湖南长沙; 广东珠海) |
| 摘 要：2-苯乙胺、反式-4-甲基环己胺分别与三光气反应生成相应的异氰酸酯。2-苯乙基异氰酸酯与3-乙基-4-甲基-3-吡咯啉-2-酮加成(收率87.2%)后,经磺化、氨解(收率78.1%)得到的取代磺酰胺,再与反式-4-甲基环己基异氰酸酯反应得到格列美脲,收率75.1%。标题化合物总收率51.1%(以吡咯啉酮计),含量99.6%(反式)。 |
| 关键词：三光气; 光气; 2-苯乙基异氰酸酯; 反式-4-甲基环己基异氰酸酯; 格列美脲; 降糖药 |
| 中图分类号：R977.1+5 文献标识码：A 文章编号：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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