联苯乙酸合成路线的研究.pdfVIP

联苯乙酸合成路线的研究 摘 要 联苯乙酸（Felbinac ）为非甾体抗消炎药，具有强消炎镇痛作用和良好的透 皮性，对治疗关节炎和肌肉疼痛具有速效，高效和安全的作用等特点。由于具有 以上优点，现在以得到广泛应用。但是目前的主要合成方法大都存在成本过高， 产率低，三废排放量大等缺点。论文研究了从对溴苯乙酮和苯硼酸为起始原料， 在四（三苯基膦）合钯做催化剂，四氢呋喃做溶剂，在碱性条件下，发生Suzuki 反应，偶合生成联苯乙酮。生成的联苯乙酮发生Willgerodt 反应，即在硫和吗啉 的中加热回流8h，再在NaOH 的乙醇溶液中水解得到联苯乙酸。Suzuki 反应产 率可达到95% 以上，Willgerodt 反应产率可达50%左右，这样总产率可达到45% 以上，与以前报道的合成方法相比，具有原料便宜，产率高，合成方法简单，废 弃物排放少，反应条件温和，容易操作，产品纯度好等优点。 关键词：Suzuki 反应，Willgerodt 反应，联苯乙酸，联苯乙酮，产率 I 联苯乙酸合成路线的研究 Abstract Felbinac is a kind of NSAIDS, which has the strong diminish inflammation abirritation and has the finer breathe freely nature, and it is quick-resulted, high-effect and safe to cure arthritis and muscleache. It has been applied abroad nowadays because of the merits above. But nowadays the disadvantages such as high-cost, low- yield , large amounts of exhaust emission almost exist in the main synthesis method .The paper in detail discusses that bromine hypnone and benzene boracic acid which are the initiative raw material happen the Suzuki reaction in the condition of alkalescence,with the Pd(pph ) as catalyst and Tetrahydrofuran as impregnant, and 3 4 create coupling bi-hypnone .Then, bi-hypnone happen the willgerodt reaction , and the process is putting the bi-hypnone into the sulfur and morpholine.To heat refluxed for eight hours, thent to hydrolyze for receiving biphenyl acetic acid from NaOH ethanol solution. The Suzuki reaction’s produce rate can reach upwards of 95 percents and the willgerodt reaction’s can reach to about 50 percents, so the overall produce rate can reach upwards of 45 percents. This reaction has the advantages such as the cheap starting materials, high-yield, the simple synthesis methods, small amounts of castoff letting , the