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本文报导合成了硝基呋喃丙烯酰胺及其酯类衍生物107个.这类化合物的合成是从糠醛經Perkin反应制备β-呋喃丙烯酸,然后硝化成β-(5-硝基-2-呋喃)丙烯酸,再經酰氯与相应的胺类或氨基酸等縮合为酰胺。酯类则直接用酸与相应的醇酯化而得.經动物篩选后发現其中有33个化合物对感染日本血吸虫病小白鼠有显著作用.尤以β-(5-硝基-2-呋喃)丙烯酰异丙胺(I_4,F-30066)及β-(5-硝基-2-呋喃)丙烯酰甘氨酸乙酯(Ⅵ_(17),F-30069)具有强烈杀虫效力,均已試用于临床,証明有一定疗效。
This paper reports the synthesis of nitrofurans acrylamide and its ester derivatives 107. The synthesis of these compounds is the preparation of β-furan acrylic acid from the furfural Perkin reaction, and then nitrated into β- (5-nitro-2-furan) Acrylic acid, followed by acid chloride and the corresponding amine or amino acid condensation to amide. Esters were directly esterified with the acid and the corresponding alcohol obtained by animal screening found that 33 of them have a significant role in the infection of Schistosoma japonicum mice, especially β- (5-nitro-2- Furan) acryloyl isopropylamine (I_4, F-30066) and β- (5-nitro-2-furan) acryloyglycine ethyl ester (Ⅵ_ (17), F-30069) In clinical, to prove that there is a certain effect.