公开(公告)号：US20210346375A1

公开(公告)日：2021-11-11

申请号：US17280637

申请日：2019-09-18

Applicant: Novartis AG

Inventor： Zhongbo Fei ,  Gang LU ,  Yinbo Wan ,  Jianhua Wang ,  Quanbing WU ,  Hao Zhang

IPC: A61K31/497 ,  C07D491/107 ,  A61K45/06

Abstract: The invention relates to a method for the manufacture of a compound of Formula I as mentioned above, or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II with a compound of the formula III according to the following reaction scheme: wherein A, LG, n and m are as defined in the Summary of the Invention.

公开(公告)号：US20200239461A1

公开(公告)日：2020-07-30

申请号：US16635596

申请日：2018-08-01

Applicant: Novartis AG

Inventor： Like CHEN ,  Chi Ming CHEUNG ,  Zhongbo FEI ,  Qun JIANG ,  Lei LI ,  Bin LI ,  Thomas RUCH ,  Hao WANG ,  Quanbing WU

IPC: C07D417/14

Abstract: The present invention provides a process of synthesizing 1-(((Z)-(1-(2-aminothiazol-4-yl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-yl)methyl)-1-sulfoazetidin-3 yl)amino)ethylidene)amino)oxy)cyclopropanecarboxylic acid (referred to herein as Compound X), or a salt thereof, or a solvate including hydrate thereof, and/or intermediates thereof, and the use of intermediates for preparing Compound X. In particular, the process relates to the preparation of Compound X using dynamic kinetic resolution (DKR) and asymmetric catalytic reduction, thereby providing an improved route to 1-(((Z)-(1-(2-aminothiazol-4-yl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-yl)methyl)-1-sulfoazetidin-3 yl)amino)ethylidene)amino)oxy)cyclopropanecarboxylic acid (Compound X) and compositions containing said compound, including the arginine salt, sodium salt and hydrated solid forms of Compound X.