多样性导向的合成塔莫西芬类型四位置换的烯
Kenichiro Itami1, Toshiyuki Kamei, Jun-ichi Yoshida
1Department of Synthetic Chemistry and Biological Chemistry, Graduate School of Engineering, Kyoto University, Nishikyo-ku, Kyoto 615-8510, Japan.
Journal of the American Chemical Society
|December 4, 2003
概括
一种新的铜催化方法可以合成他莫西芬类型的四位置换烯酸. 这种方法可以对立体化学进行精确控制,并引入对抗雌激素活性至关重要的多种基.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
背景情况:
- 塔莫西芬是治疗雌激素受体阳性乳腺癌的关键药物.
- 开发高效的合成路径,以调性质的他莫西芬类型,对于药物发现至关重要.
研究的目的:
- 开发一种新的多功能合成策略,用于他莫西芬类型的四位置换烯酸.
- 为了使基替代物的容易变化和对结构-活性关系研究的立体化学的控制.
主要方法:
- 铜催化碳磁化基基基基基基基基基基基.
- 序列添加酸以引入多种不同的替代剂.
- 替代烯的区域和立体选择性合成.
主要成果:
- 建立了一个通用合成方案,用于他莫西芬类型的四位置换烯酸.
- 该方法允许制备各种电子和结构多样化的烯酸.
- 对于抗雌激素活性至关重要的关键基组,可以很容易地从易于获得的基化物中变化.
- 通过改变酸添加的顺序,可以访问立体和区域异构体.
结论:
- 开发的Cu-催化碳磁化提供了一种强大而灵活的方法来合成他莫西芬类似物.
- 这种方法促进了以多样性为导向的合成和为药理学评估准备特定异构体.
- 合成策略对发现新的抗雌激素化合物充满希望.
相关概念视频
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Structural Isomerism
Isomerism in Complexes
Isomers are different chemical species that have the same chemical formula. Structural isomerism of coordination compounds can be divided into two subcategories, the linkage isomers and coordination-sphere isomers.
Linkage isomers occur when the coordination compound contains a ligand that can bind to the transition metal center through two different atoms. For example, the CN− ligand can bind through the carbon atom or through the nitrogen atom. Similarly, SCN− can be...
Isomers are different chemical species that have the same chemical formula. Structural isomerism of coordination compounds can be divided into two subcategories, the linkage isomers and coordination-sphere isomers.
Linkage isomers occur when the coordination compound contains a ligand that can bind to the transition metal center through two different atoms. For example, the CN− ligand can bind through the carbon atom or through the nitrogen atom. Similarly, SCN− can be...
Stereoisomerism
Isomerism in Complexes
Isomers are different chemical species that have the same chemical formula.
Transition metal complexes often exist as geometric isomers, in which the same atoms are connected through the same types of bonds but with differences in their orientation in space. Coordination complexes with two different ligands in the cis and trans positions from a ligand of interest form isomers. For example, the octahedral [Co(NH3)4Cl2]+ ion has two isomers (Figure 1) In the cis...
Isomers are different chemical species that have the same chemical formula.
Transition metal complexes often exist as geometric isomers, in which the same atoms are connected through the same types of bonds but with differences in their orientation in space. Coordination complexes with two different ligands in the cis and trans positions from a ligand of interest form isomers. For example, the octahedral [Co(NH3)4Cl2]+ ion has two isomers (Figure 1) In the cis...
Valence Bond Theory
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Transformers can provide desired voltages to a circuit by modifying the number of turns in the secondary windings.
If the ratio of the number of turns in the secondary winding to that of the primary winding is greater than one, then the transformer is said to be a step-up transformer. In a step-up transformer, the voltage at the secondary winding is greater than the voltage applied at the primary winding.
However, if this ratio is less than one, the transformer is said to be a step-down...
If the ratio of the number of turns in the secondary winding to that of the primary winding is greater than one, then the transformer is said to be a step-up transformer. In a step-up transformer, the voltage at the secondary winding is greater than the voltage applied at the primary winding.
However, if this ratio is less than one, the transformer is said to be a step-down...


