通过一种新的对轴性性双基与性转移的新型选方法对A-240610.0进行非对称合成
Yi-Yin Ku1, Tim Grieme, Prasad Raje
1D-R450, Process Chemistry, Global Pharmaceutical Research and Development, Abbott Laboratories, North Chicago, Illinois 60064-4000, USA. yiyin.ku@abbott.com
Journal of the American Chemical Society
|April 19, 2002
概括
研究人员开发了一种新的方法,用于使用性转移进行以人为选择的二甲基合成. 这种技术有效地产生了一个单一的体,使A-240610.0.0.的不对称合成成为可能.
科学领域:
- 有机化学 有机化学
- 不对称的合成方法
背景情况:
- 轴性性双是药品和材料中的重要结构图案.
- 为它们的立体选择性合成开发高效的方法仍然是一个挑战.
研究的目的:
- 开发一种新的选方法,用于制备轴性性 biaryls.
- 为了实现高立体选择性和产量在合成一个特定的atropisomer.
- 将这种方法应用于A-240610.0.0.的不对称合成.
主要方法:
- 从二次酒精立体中心向二轴转移性.
- 区域选择性的分子内基团迁移.
- 目标体的分离和表征.
主要成果:
- 成功开发了一种新型的人体选择性二醇制备方法.
- 一个单个基体 (2) 的制备,其产量为85%和99:1的二元选择性.
- 实现了A-240610.0的高效不对称合成.
结论:
- 开发的方法提供了一条高效的途径,以高立体控制的atropisomers.
- 这种方法促进了复杂分子的合成,如A-240610.0.0.
- 性转移策略是不对称合成中的一个有价值的工具.
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