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Identification and characterization of potential impurities in raloxifene hydrochloride.

作者信息

Reddy Reguri Buchi, Goud Thirumani Venkateshwar, Nagamani Nagabushanam, Kumar Nutakki Pavan, Alagudurai Anandan, Murugan Raman, Parthasarathy Kannabiran, Karthikeyan Vinayagam, Balaji Perumal

机构信息

Chemical Research & Development, NPNC Division, Orchid Chemicals and Pharmaceutical Limited, Sozhanganallur, Chennai 600 119, Tamilnadu, India.

出版信息

Sci Pharm. 2012 Jul-Sep;80(3):605-17. doi: 10.3797/scipharm.1204-13. Epub 2012 May 22.

DOI:10.3797/scipharm.1204-13
PMID:23008809
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3447609/
Abstract

During the synthesis of the bulk drug Raloxifene hydrochloride, eight impurities were observed, four of which were found to be new. All of the impurities were detected using the gradient high performance liquid chromatographic (HPLC) method, whose area percentages ranged from 0.05 to 0.1%. LCMS was performed to identify the mass number of these impurities, and a systematic study was carried out to characterize them. These impurities were synthesized and characterized by spectral data, subjected to co-injection in HPLC, and were found to be matching with the impurities present in the sample. Based on their spectral data (IR, NMR, and Mass), these impurities were characterized as Raloxifene-N-Oxide [Impurity: 1]; EP impurity A [Impurity: 2]; EP impurity B [Impurity: 3]; Raloxifene Dimer [Impurity: 4]; HABT (6-Acetoxy-2-[4-hydroxyphenyl]-1-benzothiophene or 6-Hydroxy-2-[4-acetoxyphenyl]-1-benzothiophene) [Impurity: 5]; PEBE (Methyl[4-[2-(piperidin-1-yl)ethoxy]]benzoate) [Impurity: 6]; HHBA (1-[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]ethanone) [Impurity: 7]; 7-MARLF (7-Acetyl-[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl][4-[2-(piperidin-1-yl)ethoxy]phenyl methanone) [Impurity: 8]; of which impurities 5-8 are reported for the first time.

摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a23/3447609/cc6bb99f236a/scipharm-2012-80-605f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a23/3447609/626ef89d5a09/scipharm-2012-80-605f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a23/3447609/09dfe645b2e7/scipharm-2012-80-605f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a23/3447609/02a4731228ac/scipharm-2012-80-605f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a23/3447609/7918a3c11742/scipharm-2012-80-605f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a23/3447609/cc6bb99f236a/scipharm-2012-80-605f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a23/3447609/626ef89d5a09/scipharm-2012-80-605f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a23/3447609/09dfe645b2e7/scipharm-2012-80-605f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a23/3447609/02a4731228ac/scipharm-2012-80-605f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a23/3447609/7918a3c11742/scipharm-2012-80-605f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a23/3447609/cc6bb99f236a/scipharm-2012-80-605f5.jpg

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