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Two-Step Synthesis of 1,3-Disubstituted 3,4-Dihydro-4-thioxoquinazolin-2(1H)-ones from 1-Bromo-2-fluorobenzenes

  作者 Kobayashi, K; Komatsu, T; Yokoi, Y; Konishi, H  
  选自 期刊  Helvetica Chimica Acta;  卷期  2011年94-1;  页码  67-72  
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[摘要]An efficient synthesis of 3-alkyl-3,4-dihydro-4-thioxobenzoquinazolin-2(1H)-ones 3 has been accomplished in two steps and in satisfactory yields from 1-bromo-2-fluorobenzenes 1. Thus, the reaction of 1-fluoro-2-lithiobenzenes, generated by the Br/Li exchange between 1 and BuLi, with alkyl isothiocyanates, gives N-alkyl-2-fluorobenzothioamides 2, which, in turn, react with a series of isocyanates in the presence of NaH to give the desired products 3.

 
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