公开(公告)号：US08871930B2

公开(公告)日：2014-10-28

申请号：US13989643

申请日：2011-11-16

申请人： Xinyu Zhang ,  Jiankang Xu

发明人： Xinyu Zhang ,  Jiankang Xu

IPC分类号： C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D401/14 ,  C07D401/04

CPC分类号： C07D401/14 ,  C07D401/04

摘要： Disclosed is a preparation method of α-imatinib mesylate. The reaction temperature of the method is low and the yield of the crystal is improved. Furthermore, the method is applicable to the industrial production.

摘要翻译： 公开了甲磺酸α-伊马替尼的制备方法。 该方法的反应温度低，晶体的产率提高。 此外，该方法适用于工业生产。

公开(公告)号：US20130245258A1

公开(公告)日：2013-09-19

申请号：US13989643

申请日：2011-11-16

申请人： Xinyu Zhang ,  Jiankang Xu

发明人： Xinyu Zhang ,  Jiankang Xu

IPC分类号： C07D401/14

CPC分类号： C07D401/14 ,  C07D401/04

摘要： Disclosed is a preparation method of α-imatinib mesylate. The reaction temperature of the method is low and the yield of the crystal is improved. Furthermore, the method is applicable to the industrial production.

摘要翻译： 公开了甲磺酸α-伊马替尼的制备方法。 该方法的反应温度低，晶体的产率提高。 此外，该方法适用于工业生产。

公开(公告)号：US20130225839A1

公开(公告)日：2013-08-29

申请号：US13881676

申请日：2011-10-26

申请人： Jiankang Xu ,  Meiqi Ye ,  Bin Chen ,  Qiaoqiao Xu

发明人： Jiankang Xu ,  Meiqi Ye ,  Bin Chen ,  Qiaoqiao Xu

IPC分类号： C07F9/655

CPC分类号： C07F9/65515

摘要： Preparation method of fosamprenavir derivatives is disclosed. The compound shown by formula II or its ammonium salt is reacted with a metal ion source in solvent to obtain the compound shown by formula Iii. After isolating and purifying, the compound shown by formula III is catalytically reduced to the compound shown by formula I. In the formula, X is metal ion. Preferably, the metal ion source is a calcium ion source, sodium ion source, or potassium ion source, and X is calcium ion, sodium ion, or potassium ion. The solvent is methanol, ethanol, n-propanol, isopropanol, n-butanol, or sec-butanol. The catalytic reduction is carried out by using hydrogen as a reducing agent in the presence of palladium on carbon catalyst. The ammonium salt is methylamine salt, dimethylamine salt, ethylamine salt, diethylamine salt, isopropylamine salt, dibutylamine salt, dipropylamine salt, t-butylamine salt, or dicyclohexylamine salt. The relevant intermediate of fosamprenavir derivatives in the preparation method is also provided. The preparation method of fosamprenavir derivatives reduces the cost, improves the productivity, and is applicable for large-scale popularization and application.

摘要翻译： 披露了福沙那韦衍生物的制备方法。 式II化合物或其铵盐与溶剂中的金属离子源反应得到式Iii所示的化合物。 分离纯化后，将式III化合物催化还原成式I所示的化合物。在该式中，X是金属离子。 优选地，金属离子源是钙离子源，钠离子源或钾离子源，X是钙离子，钠离子或钾离子。 溶剂是甲醇，乙醇，正丙醇，异丙醇，正丁醇或仲丁醇。 催化还原通过在钯/碳催化剂存在下使用氢作为还原剂进行。 铵盐是甲胺盐，二甲胺盐，乙胺盐，二乙胺盐，异丙胺盐，二丁胺盐，二丙胺盐，叔丁胺盐或二环己胺盐。 还提供了制备方法中福沙那韦衍生物的相关中间体。 福沙那韦衍生物的制备方法降低成本，提高生产率，适用于大规模普及应用。

公开(公告)号：US08592625B2

公开(公告)日：2013-11-26

申请号：US12811418

申请日：2008-01-02

申请人： Jiankang Xu ,  Da Zhang ,  Meiqi Ye ,  Jie Chen ,  Yongbing Guo ,  Yongjiang Hu

发明人： Jiankang Xu ,  Da Zhang ,  Meiqi Ye ,  Jie Chen ,  Yongbing Guo ,  Yongjiang Hu

IPC分类号： C07C227/36

CPC分类号： C07C227/34 ,  C07C229/08

摘要： The present invention relates to a process for resolving S-3-(Aminomethyl)-5-methylhexanoic acid, which adopts benzoyl-L-glutamic acid, 4-methyl benzoyl-L-glutamic acid, benzene sulfonyl-L-glutamic acid or 4-methyl benzene sulfonyl-L-glutamic acid as a resolution agent to make a first resolution to racemic 3-aminomethyl-5-methylhexanoic acid, and adopts the resolution agent same to that of the first resolution to make a second resolution to the first resolution product to obtain the second resolution product, thus the resolution salt product is obtained, and further hydrolyzed by an acid, the resolution agent is extracted to be separated, the pH is adjusted to be neutral, the product S-3-(Aminomethyl)-5-methylhexanoic acid, i.e. the pregabalin, is then precipitated by distillation, therefore the present invention has the characteristics of polluting the environment slightly, high efficiency and stability, simpleness and practicality, producing product with high purity and a low production cost, and is suitable for large-scale production.

摘要翻译： 本发明涉及一种分离S-3-（氨基甲基）-5-甲基己酸的方法，该方法采用苯甲酰基-L-谷氨酸，4-甲基苯甲酰基-L-谷氨酸，苯磺酰基-L-谷氨酸或4 甲基苯磺酰基-L-谷氨酸作为拆分剂，首先拆分为外消旋的3-氨基甲基-5-甲基己酸，并采用与第一分辨率相同的分解剂，以第一分辨率作第二分辨率 得到第二分解产物，得到分解盐产物，并进一步用酸水解，提取分离剂分离，将pH调节为中性，产物S-3-（氨基甲基） - 5-甲基己酸，即普瑞巴林，然后通过蒸馏沉淀，因此本发明具有污染环境的特点，效率高，稳定性，简便性和实用性，生产高纯度，低产品的产品 离子成本，适合大规模生产。

公开(公告)号：US20110098502A1

公开(公告)日：2011-04-28

申请号：US12811418

申请日：2008-01-01

申请人： Jiankang Xu ,  Da Zhang ,  Meiqi Ye ,  Jie Chen ,  Yongbing Guo ,  Yongjiang Hu

发明人： Jiankang Xu ,  Da Zhang ,  Meiqi Ye ,  Jie Chen ,  Yongbing Guo ,  Yongjiang Hu

IPC分类号： C07C227/36

CPC分类号： C07C227/34 ,  C07C229/08

摘要： The present invention relates to a process for resolving S-3-(Aminomethyl)-5-methylhexanoic acid, which adopts benzoyl-L-glutamic acid, 4-methyl benzoyl-L-glutamic acid, benzene sulfonyl-L-glutamic acid or 4-methyl benzene sulfonyl-L-glutamic acid as a resolution agent to make a first resolution to racemic 3-aminomethyl-5-methylhexanoic acid, and adopts the resolution agent same to that of the first resolution to make a second resolution to the first resolution product to obtain the second resolution product, thus the resolution salt product is obtained, and further hydrolyzed by an acid, the resolution agent is extracted to be separated, the pH is adjusted to be neutral, the product S-3-(Aminomethyl)-5-methylhexanoic acid, i.e. the pregabalin, is then precipitated by distillation, therefore the present invention has the characteristics of polluting the environment slightly, high efficiency and stability, simpleness and practicality, producing product with high purity and a low sproduction cost, and is suitable for large-scale production.

摘要翻译： 本发明涉及一种分离S-3-（氨基甲基）-5-甲基己酸的方法，该方法采用苯甲酰基-L-谷氨酸，4-甲基苯甲酰基-L-谷氨酸，苯磺酰基-L-谷氨酸或4 甲基苯磺酰基-L-谷氨酸作为拆分剂，首先拆分为外消旋的3-氨基甲基-5-甲基己酸，并采用与第一分辨率相同的分解剂，以第一分辨率作第二分辨率 得到第二分解产物，得到分解盐产物，并进一步用酸水解，提取分离剂分离，将pH调节为中性，产物S-3-（氨基甲基） - 然后通过蒸馏沉淀5-甲基己酸，即普瑞巴林，因此本发明具有轻微，高效和稳定，简单和实用的污染环境的特点，生产高纯度和低产量的产品 成本高，适合大规模生产。