934264-38-7Relevant academic research and scientific papers
Identification, synthesis, and strategy for minimization of potential impurities in the preclinical anti-HBV drug Y101
Hu, Zhanxing,An, Qiao,Li, Kunfeng,Zhang, Yangong,Qiu, Jingying,Xu, Bixue,Pan, Weidong,Cao, Peixue,Liu, Changxiao,Huang, Zhengming,Xia, Wen,Liang, Guangyi
, p. 1156 - 1167 (2013)
The identification of actual, potential, and theoretical impurities of N-[N-benzoyl-O-(2-dimethylaminoethyl)-l-tyrosyl]-l-phenylalaninol (Y101), a preclinical anti-HBV drug, is described in this article. The impurities were monitored by HPLC, and their structures were established on the basis of NMR, IR, and MS. Most of the impurities were synthesized, and their assigned constitutions were confirmed by HPLC co-injection with an ordinary column (Phenomenex Gemini, 250 mm × 4.6 mm, 5 μm) or a chiral column (DAICEL Chiralcel OD-H). According to the synthetic route, the origins of all of these related impurities were analyzed, and some practical strategies were applied for minimizing these impurities to the level accepted by the International Conference on Harmonization (ICH), and therefore, these strategies can be well applied to the quality control in Y101 clinical sample manufacture.
Development of a practical and scalable synthesis of anti-HBV drug Y101
Hu, Zhan-Xing,Zhang, Yan-Gong,An, Qiao,Xu, Bi-Xue,Pan, Wei-Dong,Cao, Pei-Xue,Liu, Chang-Xiao,Huang, Zheng-Ming,Xia, Wen,Qiu, Jing-Ying,Liang, Guang-Yi
, p. 9592 - 9600 (2015/01/08)
The process research and development of a practical and scalable synthetic method towards Anti-HBV Drug N-[N-benzoyl-O-(2-dimethylaminoethyl)-l-tyrosyl]-l-phenylalaninol (Y101) was described. Initial synthetic routes of Y101 in milligram quantities were unsuitable for large-scale synthesis to provide bulk material. As part of the collaboration between Medicinal Chemistry and Research active pharmaceutical ingredient (API), a fit for purpose route for the kilo scale synthesis of Y101 was developed. In contrast, the improved route described here did not require purification by column chromatography for all steps, and the formation of impurities was effectively suppressed. This highly efficient and scalable process was successfully demonstrated in the large-scale synthesis of Y101.
