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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
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通过使用实用的印基模板进行远程meta-selective C-H 烯化进行宏循环化
Pengfei Zhang1, Zhiwei Jiang1, Zhoulong Fan2
1College of Chemistry, State Key Laboratory of Elemento-organic Chemistry, Nankai University Tianjin 300071 China zjin@nankai.edu.cn.
Chemical science
|August 11, 2023
概括
这项研究提出了一种新的催化方法,通过C-H激活合成宏环化合物. 这种高效的策略使得可以制造宏化物,氨酸和抗瘤药物贝利诺斯塔特.
科学领域:
- 有机化学 有机化学
- 催化剂是一种催化剂.
- 药用化学 医学化学
背景情况:
- 通过C-H激活合成宏环化合物具有挑战性.
- 开发高效和多功能的宏循环化策略至关重要.
研究的目的:
- 开发一种新的催化宏循环化策略.
- 为了证明各种宏环化合物的合成,包括宏化物,氨酸和抗瘤药物贝利诺斯塔特.
- 探索铜酸盐和分子氧气作为氧化剂的使用.
主要方法:
- 帕拉催化远程甲基-C-H的olefination使用一个印度模板.
- 内部分子和分子间的C-H化反应.
- 在现场监测使用福里埃变换红外光谱和ESI-MS.
主要成果:
- 通过Pd催化后的甲基-C-H烯化开发了一种高效的宏循环化策略.
- 该方法成功合成了宏化物和氨酸.
- 从简单的前体中,分子间的化产生了抗瘤药物贝利诺斯塔特.
- 酸铜和O2取代了银盐作为氧化剂.
- 首次检测到一个环酸中间体.
结论:
- 开发的战略提供了一个有效的途径,以各种宏循环化合物.
- 这种方法为合成复杂分子,包括药品提供了一种实际的方法.
- 使用铜和氧作为氧化剂提供了一个更绿色的替代方案.
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