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公开(公告)号：US20230212212A1
公开(公告)日：2023-07-06
申请号：US18066867
申请日：2022-12-15
发明人： Chenchen HU , Qiang ZHAO , Qing LI , Jimin YANG
摘要： Disclosed are processes for preparing oligonucleotides. The process comprises: (a) converting a compound of Formula X-1 into a compound of Formula X-2: where R10 is a residue of an oligonucleotide (e.g., a phosphorodiamidate morpholino oligomer); R11 is an amine protecting group; wherein the compound of Formula X-1 is not bound to a solid support; and; (b) optionally removing protecting groups in the compound of Formula X-2 to obtain the olignucleotide. The synthetic processes described herein are advantageous in many aspects, including but not limited to improved yields and purities of target phosphorodiamidate morpholino oligomers with reduced 4-nitrostyrene adduct impurities. (X-1), (X-2)
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2.发明公开公开(公告)号：US20240158432A1
公开(公告)日：2024-05-16
申请号：US18514386
申请日：2023-11-20
发明人： Hu CHENG , Chenchen HU , Jiaxin SONG , Yang LIU , Tingting QIAN , Xianzhe WANG , Jimin YANG
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： A composition comprising dichloroacetic acid and glyoxylic acid, wherein, the content of glyoxylic acid is below 1000 pm, and the preparation method and application of the composition. A process for preparing the composition, comprising: mixing a dichloroacetic acid material having greater than 1000 ppm glyoxylic acid with a glyoxylic acid capture reagent, and a process for preparing oligonucleotides, comprising using the composition. It is found that glyoxylic acid is an impurity in commercially available DCA products, which may cause the oligonucleotides synthesis failure. Ion chromatography can be used to detect glyoxylic acid in dichloroacetic acid and accurately determine its concentration.
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3.发明授权公开(公告)号：US11873318B2
公开(公告)日：2024-01-16
申请号：US17870551
申请日：2022-07-21
发明人： Hu Cheng , Chenchen Hu , Jiaxin Song , Yang Liu , Tingting Qian , Xianzhe Wang , Jimin Yang
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： Disclosed is a composition comprising dichloroacetic acid, a process for preparing the same and a use thereof. It has been discovered that the novel impurity is glyoxylic acid, and glyoxylic acid in dichloroacetic acid can be detected and its concentration accurately measured, by ion chromatography method.
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4.发明申请公开(公告)号：US20230002438A1
公开(公告)日：2023-01-05
申请号：US17870551
申请日：2022-07-21
发明人： Hu CHENG , Chenchen Hu , Jiaxin SONG , Yang LIU , Tingting QIAN , Xianzhe WANG , Jimin YANG
IPC分类号： C07H21/00
摘要： Disclosed is a composition comprising dichloroacetic acid, a process for preparing the same and a use thereof. It has been discovered that the novel impurity is glyoxylic acid, and glyoxylic acid in dichloroacetic acid can be detected and its concentration accurately measured, by ion chromatography method.
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