利用原位红外技术指导雷帕霉素中 31/42-OH 的选择性取代。
Selective substitution of 31/42-OH in rapamycin guided by an in situ IR technique.
机构信息
Key Laboratory of Structure-Based Drug Design and Discovery, Shenyang Pharmaceutical University, Ministry of Education, Shenyang 110016, China.
Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China.
出版信息
Molecules. 2014 Jun 10;19(6):7770-84. doi: 10.3390/molecules19067770.
An in situ IR technique was applied in the selective synthesis of the key intermediate for rapamycin derivatives, which made the reaction endpoint easily defined. This technology solved a bothersome problem in the preparation of rapamycin derivatives, and based on this technique, the 31-OH and 42-OH of rapamycin were chemically modified by a series of quaternary ammonium salts to generate 11 compounds. The solubility of all these compounds was remarkably improved (25,000 times higher than that of rapamycin) and their structures were confirmed by MS, IR, 1D and 2D NMR techniques.
原位红外技术应用于雷帕霉素衍生物关键中间体的选择性合成，使反应终点易于确定。该技术解决了雷帕霉素衍生物制备中的一个难题，在此技术基础上，用一系列季铵盐对雷帕霉素的 31-OH 和 42-OH 进行了化学修饰，生成了 11 个化合物。所有这些化合物的溶解度都显著提高（比雷帕霉素高 25000 倍），其结构通过 MS、IR、1D 和 2D NMR 技术得到确认。
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