臺灣博碩士論文加值系統

2-Phenylbenzothiazole是已知具有生物活性的天然物，其衍生物也在乳癌細胞、結腸癌細胞、卵巢癌細胞、腎臟癌細胞都有良好的活性。而點擊化學經常應用於藥物方面的研發，也是一種快速又有效率的一種合成方法。在本論文利用苯炔點擊化學來進行合成抗癌試劑。

2-Phenylbenzothiazoles are known natural products with biological activity. The derivatives are potential anti-cancer activity inter breast、colon、ovarian and renal cell. The click chemistry applications are in the drug discovery, and also fast and practical synthetic method In this study, we use the aryne click chemistry to design and synthesis anti-human agent

目錄
中文摘要------I
英文摘要-----II
一、緒論-------------1
二、文獻回顧---------3
三、合成動機--------12
四、合成途徑與結果討論-------19
五、結論----------------------31
六、實驗部份
（1）儀器--------------32
（2）試劑----------------33
（3）實驗及數據結果-----------34
六、参考文獻------------------59
七、圖譜-----------------------61
圖與表目錄
1. Fig.1、2-Phenylbenzothiazoles 、flavone和isoflavone結構與位置編號-------1
2. Fig.2、2-Phenylbenzothiazole的活性機制--------------2
3. Fig.3、Stevens發表合成2-phenylbenzothiazoles途徑----3
4. Fig.4、Stevens利用聚磷酸合成2-phenylbenzothiazoles----4
5. Fig.5、Stevens在2-phenylbenzothiazoles活性位置用氟做修
飾-----5
6. Fig.6、Mathis對六號位所修飾的化合------------6
7. Fig.7、在amine位做修飾的化合物-------------6
8. Fig.8、Bradshaw針對5F 203化合物做amine位的修飾--------7
9. Fig.9、利用99mTc對amine端作修飾-------------8
10. Fig.10、利用2-nitroimidazole derivatives對amine端的修飾----------9
11. Fig.11、Total synthesis 2-(4-aminophenyl)benzothiazole -------------10
12. Fig.12、流式細胞儀分析sub-G1的數據----------11
13. Fig.13、Larock利用[3+2] Cycloaddition of Sydnones and Arynes ----------------13
14. Fig.14、Mechanism of Cycloaddition of Sydnones and Arynes------13
15. Fig.15、Larock利用o-(Trimethylsilyl)ary triflate與azide進行click reation--------------------14
16. Fig.16、Mose利用o-(Trimethylsilyl)ary triflate與進行click reation---------------14
17. Fig.17、Biehl Using Microwave-assisted Benzyne Click Chemistry --------------------15
18. Fig.18、Structure of Linezolid and Benzotriazolyl Oxazolidinone ----------------------15
19. Fig.19、(un)substituted benzotriazolyl oxazolidinone derivatives -----------------------16
20. Fig.20、Zhu利用Cu催化合成Triazole ----------16
21. Fig.21、Butcher利用Cu催化合成Triazole ----------17
22. Fig.22、Tiwari利用CuI-mediated進行Intramolecular N-arylation ----------------------17
23. Fig.23、Synthesis and Structure of Benzotriazolyl Fluorenes --------18
24. Fig.24、4-Nitro-N-phenyl-benzamide的合成-----------19
25. Table.1、4-Nitro-N-phenyl-benzamide產率------------20
26. Fig.25、 4-Nitro-N-phenyl-thiobenzamide的合成---------20
27. Table.2、4-Nitro-N-phenyl-thiobenzamide產率-----------21
28. Fig.26、2-(4-Nitro-phenyl)-benzothiazole 的合成-------22
29. Table.3、2-(4-Nitro-phenyl)-benzothiazole產率-------22
30. Fig.27、氫化溶劑比較------------------23
31. Fig.28、2-(4-aminophenyl)benzothiazole的合成--------24
32. Table.4、2-(4-aminophenyl)benzothiazole產率----------24
33. Fig.29、Proposed of Benzothiazole Derivatives---------25
34. Table.5 條件優化--------------------25
35. Table.6 CsF當量數與溫度的變化-----------26
36. Fig.30、4-Benzothiazol-2-yl-phenyl-5-methoxy-1H-benzotriazole --27
37. Table.7、4-Benzothiazol-2-yl-phenyl-5-methoxy-1H-benzotriazole產率-------------------------------------28
38. Table.8、4-Benzothiazol-2-yl-phenyl-5-methoxy-1H-benzotriazole產率-------------------------------------29
39. Fig.31、Benzotriazole合成機制----------------30
40. Fig.32、101f之單晶繞射圖----------------40
41. Fig.33、101g之單晶繞射圖----------------41
42. Fig.34、102j之單晶繞射圖----------------54

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