Abstract

A simple one-pot synthesis of N-substituted benzimidazoles from aromatic carboxylic acids and aromatic 1,2-diamines in the presence of 1-[bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxide hexafluorophosphate/hydroxybenzotriazole (HATU/HOBT) and N,N-diisopropylethylamine in DMF at 100°C, featuring good to excellent yields and easy workup, is developed. The protocol can be scaled to gram quantities, and no chromatographic purification is required.

中文翻译：

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1- [双（二甲基氨基）亚甲基] -1 H -1,2,3-三唑并[4,5-b] 3-氧合吡啶鎓六氟磷酸盐（HATU）/羟基苯并三唑（HOBT）基N取代基的一锅法2-芳基苯并咪唑衍生物

摘要

在1- [双（二甲基氨基）亚甲基] -1 H -1,2,3-三唑[4,5 ]存在下，由芳族羧酸和芳族1,2-二胺简单地一锅合成N-取代的苯并咪唑- b ]吡啶鎓-3-氧化物六氟磷酸盐/羟基苯并三唑（HATU / HOBT）和ñ，ñ二异丙基乙胺在DMF中在100℃下，具有良好至优异的产量和容易后处理，进行显影。可以将方案缩放为克量，并且不需要色谱纯化。