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Synthesis of Bis(N-acylamidines) from Amidines and N-Acylbenzotriazoles

  作者 CLODT JULIANA ISABEL; HACK VERENA DOROTHEA; FROEHLICH ROLAND; WUERTHWEIN ERNSTULRICH  
  选自 期刊  Synthesis;  卷期  2010年-9;  页码  1485-1492  
  关联知识点  
 

[摘要]Bis(N-acylamidines) 7, linked by a spacer connected to the carboxyl groups, were synthesized in moderate to good yields from bis(N-acylbenzotriazoles) 6 and amidines 2. In contrast, the corresponding bis(carboxylic acid) chlorides were not well suited for the synthesis of the compounds 7.2-Aminothiazole gave the bisamide 8, where the amidine moieties are part of heterocyclic ring systems. Furthermore, the reaction of a bis-amidine 9 with two equivalents of N-benzoylbenzotriazole (10) gave the bifunctional N-acylamidine 11, linked to the spacer at the amidine carbon atoms. All substances were thoroughly characterized including nine X-ray diffraction studies.

 
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