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绿色试剂氯化锂在制药工艺中的应用
Applications of the Green Reagent LiCl in Pharmaceutical Technology
【摘要】 本文介绍了绿色试剂氯化锂在制药工艺中的四个应用案例,分别为氯化锂促进的位阻型Claisen缩合反应、氯化锂促进短链烷氧基钠与非活化溴代芳烃的偶联反应、Konchel型格氏试剂辅助的二步合成辅酶Q9新工艺和四甲基哌啶氯化锌氯化锂试剂的应用。将这些成功范例引入制药工艺学的教学,可以充分体现氯化锂特有的绿色化学性能及其对制药工艺进步的重大促进作用,拓展学生制药工艺学思维的广度,使之感受科学之美。
【Abstract】 In this paper,four application cases are exemplified,which involve green reagent LiCl-promoted pharmaceutical processes.The cases are concretely presented as LiCl-promoted steric hindered Claisen condensation reaction,LiCl-promoted cross-coupling reaction of short-chain sodium alkoxide with unactivated aryl bromides,Konchel-type Grignard reagent-assisted two-step route to coenzyme Q9,and the use of TMPZnCl·LiCl in the synthesis of PI3Kδinhibitor GNE-293.The introduction of the successful utilities to teaching of pharmaceutical technology would sufficiently incarnate the green specific properties of lithium chloride,as well as its significant facilitation to pharmaceutical processes.As a result,students will expand their thought breadth and firsthand feel a beauty of science.
【Key words】 Teaching of pharmaceutical technology; Lithium chloride; Specificity of lithium; Lithiumpromoted synthesis; Pharmaceutical process;
- 【文献出处】 化工高等教育 ,Higher Education in Chemical Engineering , 编辑部邮箱 ,2015年03期
- 【分类号】TQ460.4-4;G642
- 【下载频次】372