Abstract. Quinazoline derivatives have been shown to be biologically active such as afatinib. The cinnamic acid derivative is an important part of the quinazoline derivative which exerts its activity. And Cinnamic acid derivatives were prepared by the benzaldehyde derivatives and malonic acids. In this paper, four cinnamic acid derivatives were prepared. The structure was confirmed by MS and 1 H NMR. In addition, this method not only saved the reaction time, but also improved the purity of the product. The yield of the step was about 90%.
2-(4-((6-bromo-3-nitroquinolin-4-yl)amino)phenyl)-2-methylpropanenitril(7) is an important intermediate in many PI3K/mTOR inhibitors. The compound 5 was synthesized from 6-bromoquinolin-4-ol (1) and 2-(4-nitrophenyl)acetonitrile(4) through five steps including nitration, chlorination, alkylation, reduction and substitution. These structures were confirmed by 1 HNMR and MS spectrum. The synthetic method of 7 was optimized and can be used to synthesize the derivatives of NVP-BEZ235.
3-chloro-2-oxo-butyric acid ethyl ester 5 is an important intermediate in many biologically active compounds such as thiazole carboxylic acids. In this work, a rapid synthetic method for compound 5 was established. The compound 5 was synthesized from the commercially available diethyl oxalate through two steps including nucleophilic substitution, chlorinated. The structure was confirmed by MS and 1 HNMR. Furthermore, the synthetic method was optimized. The total yield of the two steps was30%
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