Novartis Ag

Quanbing Wu

Zhongbo Fei

Lei Li

Thomas Ruch

Qun Jiang

Jianhua Wang

Bin Li

Hao Zhang

Chi Ming Cheung

Hao Wang

Yinbo Wan

Like Chen

Gang Lu

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.

Process of manufacture of a compound for inhibiting the activity of SHP2, as well as products resulting from acid addition

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.

Chemical process for manufacturing monobactam antibiotic and intermediates thereof

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Changshu, China

Quanbing Wu