- Identification, characterization, synthesis and strategy for minimization of potential impurities observed in the synthesis of brivaracetam
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A first systematic impurity profile research concerning nine observed and potential process related impurities of antiepileptic drug brivaracetam is reported. Among which three (impurity G/H/I) have not been discovered or reported before, these nine impurities were monitored by HPLC, and their structures were identified on the basis of MS and NMR spectroscopy. In addition to the formation, synthesis, and characterization, strategies for minimizing these impurities to the levels accepted by ICH are also described in this report.
- Liao, Shouzhu,Chen, Hongjun,Wang, Guifei,Wu, Shuming,Yang, Zaiyou,Luo, Weihe,Liu, Zhuanfeng,Gao, Xun,Qin, Junhai,Li, Chuan-hua,Wang, Zhongqing
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- To 2 - (4 - propyl pyrrolidine -2 - one) - butyramide diastereoisomer splitting method
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The invention discloses a 2 - (4 - propyl-pyrrolidine - 2 - one) - butyramide two groups of diastereoisomer splitting method. In particular to (2 S, 4 R) - 2 - (4 - propyl-pyrrolidine - 2 - one) - d amide and (2 S, 4 S) - 2 - (4 - propyl-pyrrolidine - 2 - one) - butyramide splitting, or (2 R, 4 R) - 2 - (4 - propyl-pyrrolidine - 2 - one) - d amide and (2 R, 4 S) - 2 - (4 - propyl-pyrrolidine - 2 - one) - butyramide splitting. The invention provides the use of silica gel as the stationary phase splitting method, in order to mix the organic solvent as eluant, can obtain more separation yield is greater than or equal to 90%, optical purity>de 98% of the target compound.
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Paragraph 0038-0047
(2018/07/30)
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- 4-SUBSTITUTED PYRR0LIDIN-2-0NES AND THEIR USE
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The present invention relates to optically enriched or substantially optically pure 4-substituted-pyrrolidin-2-ones of formula (III), and their uses for the synthesis of 2-oxo-pyrrolidin-l-yl derivatives.
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Page/Page column 30-31
(2010/11/26)
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- Process for the preparation of 2-oxo-1-pyrrolidine derivatives
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The present invention relates to alternative processes for the preparation of 2-oxo-1-pyrrolidine derivatives of formula (I) Particularly, the present invention relates to alternative processes for the synthesis of levetiracetam, brivaracetam and seletracetam.
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Page/Page column 25
(2010/11/27)
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