节点文献
三光气法合成降糖药格列美脲
Synthesis of Antidiabetic Glimepiride with Triphosgene
【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)。
【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%,respectively.
【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;
【Key words】 triphosgene; phosgene; 2-phenylethyl isocyanate; trans-1-isocyanato-4-methyl cyclohexane; glimepiride; antidiabetic;
【Key words】 triphosgene; phosgene; 2-phenylethyl isocyanate; trans-1-isocyanato-4-methyl cyclohexane; glimepiride; antidiabetic;
- 【文献出处】 精细化工中间体 ,Fine Chemical Intermediates , 编辑部邮箱 ,2006年03期
- 【分类号】R914.5
- 【被引频次】4
- 【下载频次】765