Silica-Supported Polyphosphoric Acid in the Synthesis of 4-Substituted Tetrahydroisoquinoline Derivatives
作者:Stanimir Manolov、Stoyanka Nikolova、Iliyan Ivanov
DOI:10.3390/molecules18021869
日期:——
α-amidoalkylation reaction, as an alternative efficient synthesis of 4-aryl- and 4-methyl-1,2,3,4-tetrahydroisoquinoline derivatives. The amides required for this purpose would result from reaction of aminoacetaldehyde dimethylacetal with different substituted benzenes in polyphosphoric acid, followed by acylation of the obtained amines with different acid chlorides or sulfochlorides. We compared the cyclisation
我们在此报告了 α-酰胺烷基化反应的应用,作为 4-芳基-和 4-甲基-1,2,3,4-四氢异喹啉衍生物的替代有效合成。为此目的所需的酰胺将来自氨基乙醛二甲基缩醛与不同取代苯在多磷酸中的反应,然后用不同的酰氯或磺酰氯对所得胺进行酰化。我们比较了使用常规(乙酸-三氟乙酸 = 4:1 环境)和固体负载试剂 (SiO2/PPA) 的环化步骤,回收、再生和再利用时不会损失其活性催化剂。我们发现,与常规方法相比,反应收率更高,反应时间更短。