Wang Jin Zhao, Zeng Su, Hu Gong Yun, Wang Dan Hua
Department of Pharmaceutical Analysis and Drug Metabolism, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, China.
J Chromatogr A. 2009 Apr 10;1216(15):3044-7. doi: 10.1016/j.chroma.2009.01.053. Epub 2009 Jan 23.
SSS-Octahydroindole-2-carboxylic acid (SSS-Oic) is a key intermediate used in the synthesis of some angiotensin-converting enzyme (ACE) inhibitors. The separation of diastereoisomers and enantiomers of Oic was performed using a pre-column derivatization chiral HPLC method. Phenyl isothiocyanate (PITC) was used as the derivatization reagent. Three PITC derivatives of Oic stereoisomers were separated on an Ultron ES-OVM chiral column (150 mm x 4.6 mm, 5 microm). Derivatization conditions such as reaction temperature, reaction time and derivatization reagent concentration were investigated. The chromatographic conditions for separation of the three PITC-Oic derivatives were optimized. The method was successfully applied in the diastereoisomeric and enantiomeric purity test of SSS-Oic.
SSS-八氢吲哚-2-羧酸（SSS-Oic）是合成某些血管紧张素转换酶（ACE）抑制剂时使用的关键中间体。采用柱前衍生化手性高效液相色谱法对Oic的非对映异构体和对映体进行分离。使用异硫氰酸苯酯（PITC）作为衍生化试剂。在Ultron ES-OVM手性柱（150 mm×4.6 mm，5微米）上分离了Oic立体异构体的三种PITC衍生物。研究了反应温度、反应时间和衍生化试剂浓度等衍生化条件。优化了三种PITC-Oic衍生物的分离色谱条件。该方法成功应用于SSS-Oic的非对映体和对映体纯度检测。
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