摘要：近几年抗癌新药的开发有了很大的进展，药物抗癌也越来越受到重视，紫杉醇因为其具有独特的抗癌活性及作用机制而成为新一代抗癌新药的代表，但由于有过敏反应、水溶性差、神经毒性、心血管毒性等不良反应。改变其剂型与对其进行结构修饰成为更多人研究的方向。因此本论文就针对其缺点对紫杉醇的C-7和C-10进行修饰。对于其中一种衍生物2,9-二(3-羟基-2-甲基-2-羟甲基丙酰氧基-10-脱乙酰基巴卡丁Ⅲ的合成方法进行研究，期望得到治疗效果更好的成果，并分析其抗癌活性。22083
毕业论文关键词：前列腺肿瘤；抗癌；卡巴他赛；结构修饰
Synthesis of 2,9-bis(3-hydroxy-2-methyl-2-hydroxymethyl
propionyloxy) 10-Deacetylbaccatin Ⅲ
Abstract: In recent years, the development of anti-cancer drug made great progress, more and more attention of anti-cancer drugs, because paclitaxel has unique anti-cancer activity and mechanism of action, it become the representative of a new generation of anti-cancer drug. But it is invalid to cure cancer, for it can produce multi-drug tolerance ,allergic reactions, poor water solubility, neurotoxicity, cardiovascular toxicity and other adverse reactions. Changing its forms and its modified structure has become more human research direction. Therefore, this paper for its shortcomings on paclitaxel on the C7 and C10 modified. Wherein a derivative of 2,9-bis(3-hydroxy-2-methyl-2-hydroxymethyl-propionyloxy-10-DBAⅢ) Synthesis of Acetyl Chiba study the therapeutic effect desired to obtain a more good results.
Keywords: Prostate; cancer; Cabazitaxel; paclitaxel
 
目  录
1  绪论    1
2  文献综述        2
2.1  紫杉醇的简介    2
2.1.1 紫杉醇的药用价值    2
2.1.2 紫杉醇的半合成    3
2.1.3 紫杉醇的抗癌机制    4
2.2 卡巴他赛及其衍生物的研究进展    5
2.2.1  卡巴他赛简介    5
2.2.2  卡巴他赛的合成方法    5
2.2.3  卡巴他赛的结构修饰    6
2.3 实验方案确定    6
3  实验部分    10
3.1 试剂与仪器    10
3.1.1 试剂                                                       10
3.1.2 仪器                                                       11
3.2 卡巴他赛的合成     11
  3.2.1 化合物6的合成                                              11
  3.2.2 化合物8的合成                                              12
  3.2.3 化合物9的合成                                              13 2,9-二(3-羟基-2-甲基-2-羟甲基丙酰氧基）10-脱乙酰基巴卡丁Ⅲ的合成:http://www.751com.cn/yixue/lunwen_14558.html