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含二催化中心手性配体的鉴定_制药工程论文范文

发布时间:2015-04-02 来源:人大经济论坛
制药工程论文范文 目 录 中文摘要I 英文摘要II 目录III 1. 绪论1 1.1 手性化合物在医药领域的应用1 1.2 手性氨基醇的合成2 1.3 手性氨基醇在不对称催化中的应用4 1.4 外消旋化合物的拆分5 1.5 展望6 2. 实验部分7 2.1 实验仪器7 2.2 实验试剂和原料7 2.3 熔点的测定8 2.4 旋光度的测定8 2.5 本章小结8 2.6 流程图9 3. 结果与讨论10 3.1实验结果10 3.2实验讨论12 4.总结与展望14 致谢15 参考文献16 摘要:手性氨基醇在不对称合成领域中是一类重要的手性源,同时,手性氨基醇在药物合成和外消旋体拆分等领域也具有广泛的用途。本论文在查阅相关资料的基础上验证了不对称催化还原反应的研究新进展。 为寻找性能优异的催化剂,基于多催化中心配体在不对称还原反应中的协同效应,可获得手性仲醇较高的e.e.值。我们分别使用了(1R,2S)-(-)或(1S,2R)-(+)-2-氨基-1,2-二苯基乙醇为手性源与间二苄溴反应,经优化反应条件后在乙腈溶液中,于60-65℃下,以KI为催化剂,K2CO3为缚酸剂,合成了二催化中心配体:N-(1’R,2’S)-(1’,2’-二苯基-2’-羟基)和N-(1’S,2’R)-(1’,2’-二苯基-2’-羟基)乙基-间二苄胺,经硅胶柱色谱纯化得无色晶体,产率较高。产物结构经IR、MS、1HNMR等确认,在新合成的一对对映体中,其光谱性质、比旋光度等物理常数均得到很好的验证。 关键词:手性氨基醇;配体;鉴定 Abstract: Chiral amino alcohol in the field of asymmetric synthesis is a kind of important chiral source, at the same time,chiral amino alcohol has extensively applicates in drug synthesis and separation raceme with broad areas . In this paper,the inspection on the based of the relevent summarizes the asymmetric catalytic reduction of new progress. In order to find the catalytic performance,based on more catalysis center ligand in asymmetric caltalytic reduction of synergies,can achieve available chiral seconddary alcohols higher e.e. value. We were respectively using (1R, 2S )-(-) and (1S, 2R )-(+)- 2 - amino -1,2 – diphenyl ethanol as chiral sources with 1,3-benzyl bromide reponse by optimizing the reaction conditions in acetonitrile solution,in the 60-65℃,KI as a catalyst,K2CO3as a hydrogen absorption reagent first synthesized the catalysis center with the ligand: N-(1'R, 2'S) - (1 ', 2'- diphenyl -2 '- hydroxy) and N-(1'S, 2'R) - (1', 2'-diphenyl -2 '- hydroxy) ethyl -1’,3’- benzyl amine,by silica gel column chromatograp get the colorless crystal, yields are higher . Product by the IR、MS and 1HNMR,ect. Confirmed. Pairs enantiomer in the synthesis,their action spectrum character,the melting point and specific rotation etc. Other physcal constants are very good test.Keywords: Chiral Amino Alcohols; Ligand; Identification
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