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本文报道38个β-(5-硝基-2-呋喃)丙酰胺及其α,β-二溴取代衍生物的合成。这类化合物的制备是以相应的β-(5-硝基-2-呋喃)丙烯酰胺类化合物(Ⅰ)进行催化氢化或与溴加成而得。经动物筛选发现β-(5-硝基-2-呋喃)丙烯酰胺类的丙烯双键以氢饱和以后生成丙酰胺类化合物(Ⅱ),对感染日本血吸虫病的小白鼠完全失去治疗或预防作用。而以溴饱和双键的α,β-二溴化合物(Ⅲ)则仍然有较显著的杀虫作用。其中尤以β-(5-硝基-2-呋喃)-α,β-二溴丙酰异丙胺(Ⅲ_(11))和β-(5-硝基-2-呋喃)-α,β-二溴丙酰甘氨酸乙酯(Ⅲ_(24))最为显著,后者曾试用于临床,证明有一定疗效。
This paper reports the synthesis of 38 β- (5-nitro-2-furan) propanamide and its α, β-dibromo substituted derivatives. The preparation of such compounds is based on the catalytic hydrogenation or addition of bromine to the corresponding β- (5-nitro-2-furan) acrylamide compounds (I). After animal screening, it was found that the propionamide compound (II) was formed after the propylene double bond of β- (5-nitro-2-furan) acrylamide was saturated with hydrogen and completely lost the therapeutic or preventive effect on the mice infected with schistosomiasis japonica . However, the α, β-dibromo compound (Ⅲ) with saturated double bonds of bromine still has a significant insecticidal effect. Among these compounds, β - (5-nitro-2-furan) -α, β-dibromopropionamines (Ⅲ_ (11) Dibromopropionylglycine ethyl ester (Ⅲ_ (24)) the most significant, which has been tried in clinical trials to prove a certain effect.