公开(公告)号：EP4261202A1

公开(公告)日：2023-10-18

申请号：EP21902559.0

申请日：2021-12-06

申请人： GNT Pharma Co., Ltd

发明人： ZHANG, Guoqing ,  ZHUANG, Chenghan ,  WANG, Lei ,  GWAG, Byoung Joo ,  AHN, Chun San ,  JIN, Jing Yu ,  XU, Xinliang

IPC分类号： C07C229/64 ,  C07C227/42

摘要： The present invention relates to the technical field of pharmaceutical crystal forms, and specifically relates to 2-hydroxy-5-[2-(4-(trifluoromethylphenyl)ethylamino)]benzoic acid crystal forms and a preparation method therefor. Crystal form I is a monoclinic crystal system, which has a Pc space group and can be obtained by means of crystallization methods of slow cooling, evaporating the solvent at a constant temperature, evaporating the solvent at an increased temperature, or adding an anti-solvent. Crystal form II is a triclinic crystal system, which has a P1 space group and can be obtained by crystallization methods such as rapid cooling or freeze-drying. The advantages of the two crystal forms and the preparation method therefor of the present invention are as follows: 1) the process is simple, costs are low, and the yield exceeds 90%; and 2) the crystal forms of the crystal forms I and II have high purity, the crystal shapes thereof are intact, and have excellent fluidity, facilitating preparation, particularly the preparation of a pharmaceutical preparation for preventing and/or treating degenerative diseases of the central nervous system; in addition, the two crystal forms have a better apparent solubility than that of raw materials. ( Figure 1 )

公开(公告)号：EP4261201A1

公开(公告)日：2023-10-18

申请号：EP21902558.2

申请日：2021-12-06

申请人： GNT Pharma Co., Ltd

发明人： ZHUANG, Chenghan ,  WANG, Lei ,  LU, Xin ,  ZHANG, Bo ,  GWAG, Byoung Joo ,  AHN, Chun San ,  JIN, Jing Yu ,  XU, Xinliang

IPC分类号： C07C227/18 ,  C07C229/64

摘要： The present invention relates to the technical field of drug synthesis methods, and relates to a method for preparing 2-hydroxy-5-[2-(4-(trifluoromethylphenyl)ethylamino)]benzoic acid. The method comprises steps such as protection, condensation, and hydrolysis. By means of the screening of a hydroxyl protecting reagent for a starting material, i.e., 2-(4-trifluoromethyl)phenethylalcohol and the optimization of other process parameters, the contents of meta-isomer impurities and disubstituted impurities in a target product are effectively controlled, such that the quality of the product is significantly improved, the reaction yield is also greatly improved, and the improved product quality can satisfy related requirements of preparation research.