Pingili R Reddy, Jambula M Reddy, Ganta M Reddy, Ghanta M Reddy, Sajja E, Sundaram V, Boluggdu V Bhaskar
Department of Research and Development, Dr. Reddy's Laboratories Ltd., Bollaram, India.
Pharmazie. 2005 Nov;60(11):814-8.
Rabeprazole sodium (1, Achiphex) is a gastric proton pump inhibitor. It causes dose-dependent inhibition of acid secretion and is useful as an anti-ulcer agent. In the process for the preparation of 1, two potential unknown impurities were identified in HPLC at levels ranging from 0.05-0.8%. Based on mass spectral data vide LC-MS, the two impurities were characterized as 2-{[(4-chloro-3-methyl-2-pyridinyl) methyl] sulfinyl}-1H-bezimidazole (2, chloro analogue of rabeprazole) and 2-[{(4-methoxy-3-methyl-2-pyridinyl)methyl}sulfinyl]-1H-benzimidazole (3, methoxy analogue of rabeprazole). The structures were unambiguously established by independently synthesizing them and co-injecting in HPLC. To our knowledge, the compounds 2 and 3 have not been reported as process impurities elsewhere.
雷贝拉唑钠（1，商品名耐信）是一种胃质子泵抑制剂。它能引起剂量依赖性的胃酸分泌抑制，可用作抗溃疡药物。在制备1的过程中，通过高效液相色谱法（HPLC）鉴定出两种潜在的未知杂质，含量范围为0.05 - 0.8%。基于液相色谱 - 质谱联用（LC - MS）的质谱数据，这两种杂质被鉴定为2-{[(4 - 氯 - 3 - 甲基 - 2 - 吡啶基)甲基]亚磺酰基}-1H - 苯并咪唑（2，雷贝拉唑的氯类似物）和2 - [{(4 - 甲氧基 - 3 - 甲基 - 2 - 吡啶基)甲基}亚磺酰基]-1H - 苯并咪唑（3，雷贝拉唑的甲氧基类似物）。通过独立合成并在HPLC中共同进样，明确确定了它们的结构。据我们所知，化合物2和3在其他地方尚未作为工艺杂质被报道。
