384835-92-1Relevant articles and documents
Development of a Scalable Method for Manufacturing the Central Core of CD73 Inhibitor AB680
Fournier, Jeremy,Yan, Xuelei,Tran, Anh T.,Grange, Rebecca L.,Jacob, Steven D.,Kalisiak, Jaroslaw,Lawson, Kenneth V.,Connor, Eric F.,Leleti, Manmohan R.,Powers, Jay P.
, p. 157 - 162 (2021/01/09)
AB680 is a highly potent CD73 small molecule inhibitor discovered and developed by Arcus Biosciences, currently in clinical trials for the treatment of pancreatic cancer. Here, we report the development of a scalable and practical method for the manufacturing of the azaindazole central core. This synthesis features an N-oxide formation followed by an α-chlorination with POCl3 leading to the formation of 4,6-dichloro-1H-pyrazolo[3,4-b]pyridine 1 in high yield and 99.5% UV purity. This method was successfully performed on multikilogram scale to support the synthesis of AB680.
MODULATORS OF 5'-NUCLEOTIDASE, ECTO AND THE USE THEREOF
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Paragraph 0350, (2017/08/01)
Compounds that modulate the conversion of AMP to adenosine by 5'- nucleotidase, ecto, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by 5'-nucleotidase, ecto is also provided.
