高度替代的aminotetrahydropyrans的合成通过立体特异的多向量C-H功能启用
Guowei Kang1, Li-Jun Xiao1, Kevin D Hesp2
1Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Organic letters
|June 9, 2023
概括
高度替代的aminotetrahydropyrans使用顺序C-H功能化进行了合成. 这种方法可以通过催化和随后的氨基功能化来创造复杂的分子.
科学领域:
- 有机化学 有机化学
- 合成化学 合成化学
- 催化剂是一种催化剂.
背景情况:
- 氨基酸是药物化学中重要的结构动图.
- 高度替代的aminotetrahydropyrans的高效合成仍然是一个挑战.
- C-H功能化为分子构造提供了一个强大的策略.
研究的目的:
- 为高度替代的aminotetrahydropyrans开发一种新的合成途径.
- 探索复杂分子合成的顺序C-H功能化策略.
- 为了在aminotetrahydropyran核心上实现替代物的立体选择性引入.
主要方法:
- 帕拉 (II) 催化型立体选择性γ-甲基C-H氨基四基的化.
- 由此产生的初级氨基的顺序α-化或化.
- 用了一系列的酸和各种替代品用于 arylation 步骤.
主要成果:
- 通过两步序列成功合成高度替代的aminotetrahydropyrans.
- 最初的γ-C-H化过程中,与各种化进行了中度到良好的产量.
- 随后的α-功能化证明了高的 diastereoselectivity,产生增值产品.
结论:
- 序列C-H功能化为合成复杂的aminotetrahydropyrans提供了一种有效的方法.
- 开发的方法提供了一个通用的平台,可以访问各种替代的aminotetrahydropyrans.
- 这种方法有助于构建潜在的有价值的制药中间体.
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