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A Convenient Synthetic Approach to Saccharin Derivatives ­Containing a Sulfonylamidine Scaffold
Synthesis ( IF 2.2 ) Pub Date : 2018-01-11 , DOI: 10.1055/s-0036-1591882
Yantao Chen 1 , Carl-Johan Aurell 2 , Pernilla Korsgren 3 , Johanna Malm 3 , Malin Härslätt 3 , Maria Fridén-Saxin 4 , Anna Pettersen 3
Affiliation  

Abstract

A key intermediate was obtained as solid through filtration of the reaction mixture of saccharin, chloro(triphenyl)phosphonium chloride, and N,N-diisopropylethylamine (DIPEA) in chloroform. The soluble triphenylphosphine oxide went to filtrate as waste, while the solid was reacted with amines to afford N-sulfonylamidines. In total, 26 N-sulfonylamidine products were obtained in moderate to good overall yields.

A key intermediate was obtained as solid through filtration of the reaction mixture of saccharin, chloro(triphenyl)phosphonium chloride, and N,N-diisopropylethylamine (DIPEA) in chloroform. The soluble triphenylphosphine oxide went to filtrate as waste, while the solid was reacted with amines to afford N-sulfonylamidines. In total, 26 N-sulfonylamidine products were obtained in moderate to good overall yields.



中文翻译:

一种方便的合成方法,以糖精衍生物的磺酰lam啶支架。

摘要

通过过滤糖精,氯(三苯基)phosph和NN-二异丙基乙胺(DIPEA)在氯仿中的反应混合物,获得了作为固体的关键中间体。可溶性三苯膦氧化物作为废物过滤出,而固体与胺反应得到N-磺酰胺基。总共以中等至良好的总产率获得了26种N-磺酰胺基产物。

通过过滤糖精,氯(三苯基)phosph和NN-二异丙基乙胺(DIPEA)在氯仿中的反应混合物,获得了作为固体的关键中间体。可溶性三苯膦氧化物作为废物过滤出,而固体与胺反应得到N-磺酰胺基。总共以中等至良好的总产率获得了26种N-磺酰胺基产物。

更新日期:2018-01-11
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