Synthesis of new 1H-imidazoles via reactions of 3(,5)-(di)chloro-2H-1,4-(benz)oxazin-2-ones with α-aminoketones
作者:Bart P. Medaer、Georges J. Hoornaert
DOI:10.1016/s0040-4020(99)00087-3
日期:1999.3
react with α-aminoketones to yield bi- and tricyclic imidazo-fused intermediates via an intramolecular cyclisation reaction. Reaction of these lactone intermediates with various nucleophiles generates new substituted 1H-imidazoles useful for pharmacological screening. Reactions of compounds 1 with β-amino-alcohols followed by treatment with SOCl2 provides 2,3-dihydro-8H-imidazo[2,1-c]-1,4-oxazin-8-ones
3,5-二氯-2 H -1,4-恶嗪-2-酮1和3-氯-2 H -1,4-苯并恶嗪-2-酮2与α-氨基酮反应生成双环和三环咪唑-通过分子内环化反应稠合的中间体。这些内酯中间体与各种亲核试剂的反应产生了可用于药理学筛选的新的取代的1 H-咪唑。化合物1与β-氨基醇的反应,然后用SOCl 2处理,得到2,3-二氢-8 H-咪唑并[ 2,1 - c ] -1,4-恶嗪-8-酮,但内酯裂解导致一些未知的分解产物的形成。