有效的固体相合成和细分A-H,J和K的结构特征
Liangyu Liu1, Wanqiu Lu1, Quanping Guo1
1Key Laboratory of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Sciences, Lanzhou University, 199 West Donggang Road, Lanzhou 730000, China.
科学家们开发了一种新的固相合成segetalins,这是来自Vaccaria segetalis的生物活性环. 这种高效的方法允许这些重要化合物的可扩展的生产和生物评估.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 类化学 类化学
背景情况:
- 塞格塔林A-H,J和K是从Vaccaria segetalis中分离出来的生物活性环.
- 这些化合物的先前合成方法具有局限性.
研究的目的:
- 为A-H,J和K.segetalins建立一个高效和可扩展的固相合成策略.
- 为了使这些环的生物评估.
主要方法:
- 固态阶段合成 (SPPS) 使用Fmoc化学在2-三化树脂上.
- 在DMF中由PyBOP调解的头到尾循环.
- 通过逆相高性能液态染色学 (RP-HPLC) 进行净化.
主要成果:
- 实现了对A-H,J和K (1-10) 的segetalins的总合成.
- 对于所有环酸,孤立产量在45-70%之间.
- 通过HRESIMS,NMR和HPLC (>95%纯度) 确认了结构相同性.
- 循环二重化 (CD) 光谱学揭示了不同的二次结构,包括β-sheet和α-helical元素.
结论:
- 建立了一种高效,可扩展的固体相合成策略.
- 这种方法克服了以前合成方法的局限性.
- 合成的segetalins可用于进一步的生物评估.
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