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国产抗日本住血吸虫病药物呋喃丙胺[N-异丙基-β-(5-硝基-2-呋喃)丙烯酸胺],其制备方法据雷兴翰等报道,是用糠醛与乙酸酐经Perkin反应制成β-呋喃丙烯酸,再硝化成β-(5-硝基-2-呋喃)丙烯酸;后者制成酰氯后再与异丙胺缩合得到呋喃丙胺。但这合成路线制备~(14)C标记的呋喃丙胺需要过量很多的~(14)C-乙酸酐,故不适用。本文报道呋喃丙胺-1-~(14)C的合成,其设计的合成路线系先以溴乙酸乙酯-1-~(14)C(Ⅰ)与三苯基膦缩合成
Domestic anti-Japanese live schistosomiasis drug furapropylamine [N-isopropyl-β- (5-nitro-2-furan) acrylic acid amine], its preparation method reported by Lei Xinghan, is the use of furfural and acetic anhydride by Perkin The reaction is made β-furan acrylic acid, and then nitrated into β- (5-nitro-2-furan) acrylic acid; the latter is made after acid chloride condensation with isopropylamine furanpropylamine. However, the synthetic route of ~ (14) C-labeled furosemide needs an excess of ~ (14) C-acetic anhydride, so it is not suitable. In this paper, the synthesis of furosemide 1- ~ (14) C was reported. The synthetic route of this method was firstly to condense the ethyl bromoacetate -1- (14) C (Ⅰ) with triphenylphosphine