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本文报导α-取代-β-(5-硝基-2-呋喃)丙烯酰胺及酯类衍生物85个的合成。这类化合物系分别以糠醛或硝基糠醛与相应的羧酸钾盐经Perkin反应缩合后,按一般方法制成酰胺及酯;或以相应的硝基呋喃丙烯酰胺经溴化;或通过氮内酯中间体经水解、醇解和氨解而制备。经动物篩选后发现有13个化合物对感染日本血吸虫小白鼠有作用,其中α—甲基—β-(5-硝基-2-呋喃)丙烯酰正丁胺(I_6,F-30058),α-甲基-β-(5-硝基-2-呋喃)丙烯酰乙醇胺(I_(10),F-30141)及α-甲基-β-(5-硝基-2-呋喃)丙烯酰-2′-羟基丙胺(I_(11),F-30111)三个具有较好抑制作用。
This paper reports the synthesis of 85 α-substituted-β- (5-nitro-2-furan) acrylamide and ester derivatives. Compounds of this type are prepared by condensing Perf furfural or furfural with the corresponding carboxylic acid potassium salts, respectively, following Perkin reaction to form amides and esters in the usual manner; or by bromination of the corresponding nitrofurans acrylamide; or by nitrogen Ester intermediates are prepared by hydrolysis, alcoholysis and ammonolysis. Thirteen compounds were found to be effective against Schistosoma japonicum infection in mice after animal screening, in which α-methyl-β- (5-nitro-2-furan) (I_ (10), F-30141) and α-methyl-β- (5-nitro-2-furan) acryloyl -2’-hydroxypropylamine (I_ (11), F-30111) three have better inhibition.