通过动态分辨率合成富含乙的螺旋环二-烯二
Anthony Choi1, Anjan Das1, Anthony J H M Meijer1
1Department of Chemistry, University of Sheffield, Sheffield S3 7HF, UK. i.coldham@sheffield.ac.uk.
Organic & biomolecular chemistry
|February 5, 2024
概括
使用奇拉基,用高反体比率分离出奇拉式螺旋环型皮佩里丁. 这些化合物是药物发现的有价值的3D碎片,可以进一步功能化.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
背景情况:
- 螺旋环型皮佩里丁是药物化学中的重要支架.
- 开发用于它们的合成的酶选择性方法对于药物发现至关重要.
研究的目的:
- 为了实现N-Boc-spirocyclic 2-arylpiperidines的运动分辨率.
- 探索这些解决的piperidines作为药物发现中的3D片段的实用性.
主要方法:
- 动力分辨率使用奇拉基 n-丁/(-) - - 斯帕特因.
- 通过循环或金属光电氧催化剂合成皮佩里丁前体.
主要成果:
- 对于溶解的piperidines,可以达到高的反体比.
- 溶解后的化合物可以进一步功能化,而不会影响其抗纯度.
结论:
- 开发的方法可以有效地获取对酸乙酸N-Boc-spirocyclic 2-arylpiperidines的有效访问.
- 这些化合物代表了制药研究和开发的宝贵3D构建块.
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