紫杉醇C13片段_____配体;

用一种可回收的配体催化合成紫杉醇C13片段

http://www.100md.com 《第四军医大学学报》 2004年第7期

紫杉醇C13片段,,配体;,紫杉醇C13片段,0引言,1材料和方法,2结果,3讨论

     Synthesis of taxol side chain precursor with a new recoverable ligand

    JIN Ying, SUN XiaoLi, CHEN Hui, ZHANG ShengYong, CHEN Lei

    Department of Chemistry, School of Basic Medicine, Fourth Military Medical University, Xi’an 710033, China

    【Abstract】 AIM: To develop a simple and economical method to achieve taxol side chain precursor, (2R，3S)isoproplyl 3benzamido2hydroxy3phenylpropionate. METHODS: A highly enantioselective C13 side chain 2 was obtained by osmiumcatalyzed asymmetric aminohydroxylation (AA) of isopropyl transcinnamate, with Nbromobenzamide as an oxidant /nitrogen reagent in the presence of ligand 4. After reaction, diethyl ether was added and filtered and ligand was recovered. RESULTS: Total yield of C13 side chain 2 was 39%, the enantiomeric excess was 98% and recovery rate of ligand 4 was 76%. CONCLUSION: This synthetic process is simple and economical, for the ligand, better than polymersurpported ligand, can be easily prepared, recovered and reused.

    【Keywords】 ligand; taxol C13

    【摘要】目的：建立一种经济的方法合成紫杉醇C13侧链(2R ......

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