公开(公告)号：EP4375285A1

公开(公告)日：2024-05-29

申请号：EP21954827.8

申请日：2021-12-01

申请人： Asymchem Laboratories (Tianjin) Co., Ltd. ,  Jilin Asymchem Pharmaceuticals Co., Ltd.

发明人： JAMES, Gage ,  MARK, McLaws ,  ZHANG, Wenchun ,  CHEN, Chaoyong ,  JING, Dingding ,  ZHANG, Baojie ,  JIANG, Yong

IPC分类号： C07D477/20 ,  C07D477/02

摘要： The disclosure provides a new crystal form of ertapenem sodium and preparation method therefor. The new crystal form of ertapenem sodium has 27 principal characteristic peaks in an X-ray powder diffraction diagram. The crystal form of ertapenem sodium of the disclosure has a rod-like crystal habit, which has a large particle size, is not prone to aggregation and is easier to dry, and a product with high crystallinity and high purity may be obtained by simple drying treatment. Meanwhile, the crystal form of the disclosure has better stability, and the crystal form may remain unchanged to a maximum extent in subsequent washing and drying processes, thereby further improving the purity of the product.

公开(公告)号：EP3978505A1

公开(公告)日：2022-04-06

申请号：EP19950893.8

申请日：2019-10-28

申请人： Jilin Asymchem Pharmaceuticals Co., Ltd.

发明人： HONG, Hao ,  JAMES, Gage ,  CHEN, Chaoyong ,  LU, Jiangping ,  JIANG, Yong ,  TAO, Jian ,  LUO, Yong

IPC分类号： C07F9/6561 ,  B01J31/22

摘要： The present invention discloses a continuous preparation method for a penem intermediate MAP. The continuous preparation method includes the following steps: step S1, in a column-type continuous reactor, using a rhodium-loaded catalyst to catalyze 4-nitrobenzyl(R) -2-diazo-4-((2R,3S)-3-((R)-1-hydroxyethyl)-4-oxoazetidin-2-yl)-3-oxopentanoate to generate a cyclization reaction so as to form a first intermediate, herein the rhodium-loaded catalyst is loaded in the column-type continuous reactor, and the rhodium-loaded catalyst has the following structural formula: (P-COO)- x Rh 2 (OOCR 1 ) 4-x ; step S2, performing an esterification reaction on the first intermediate, a diphenyl chlorophosphate and a diisopropylethylamine in a second continuous reactor, to obtain a product system containing the penem intermediate MAP; and step S3, performing crystallization treatment on the product system, to obtain the penem intermediate MAP. The column-type continuous reactor and the rhodium-loaded catalyst enable the cyclization reaction to perform efficiently at a lower temperature, thereby the energy consumption is reduced