自行车[m.n.k]构建块作为有前途的二和自行车异体:多重组合成,物理化学和结构特征
Volodymyr V Semeno1,2, Vadym O Vasylchenko1, Ihor M Fesun1
1Enamine Ltd., Chervonotkatska Street 78, Kyїv, 02094, Ukraine.
Chemistry (Weinheim an der Bergstrasse, Germany)
|December 27, 2023
概括
一种新的电友双键功能化方法可以有效地合成多种多样性的bicyclo[m.n.k]alkanes. 这些化合物在药物化学中充当有价值的构建块和潜在的异体.
科学领域:
- 有机化学 有机化学
- 合成方法论 合成方法论
- 药用化学 医学化学
背景情况:
- 自行车支架在制药中很普遍.
- 开发高效的合成路径到多样化的自行车结构仍然是一个挑战.
研究的目的:
- 开发一种通用的方法来合成桥接和合的双环[m.n.k]衍生物.
- 确定开发的合成序列的范围和局限性.
- 准备用于药物化学应用的新型构建块.
主要方法:
- 电友双键功能化与分子内酸化相结合.
- 对反应范围和局限性的系统评估.
- 目标双循环化合物的多重克尺度合成.
主要成果:
- 成功合成了一系列的cyclo[m.n.k],包括bicyclo[4.1.1]octanes,bicyclo[2.2.1]heptanes,bicyclo[3.2.1]octanes,bicyclo[3.1.0]hexanes,以及bicyclo[4.2.0]heptanes.这些的组成部分.
- 准备了50多个单一和双功能构建块.
- 已被证明适用于多重图合成.
结论:
- 开发的方法提供了对各种单环化合物的有效访问.
- 合成的化合物显示为和环环的异体具有前途.
- 物理化学和结构特征支持它们在药物发现方面的潜力,并为未来的异替代药物研究提出了指导方针.
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