Extracurricular laboratory: Synthetic route of 22468-26-4

The article 《Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952》 also mentions many details about this compound(22468-26-4)Category: chiral-catalyst, you can pay attention to it, because details determine success or failure

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 4-Hydroxypicolinic acid(SMILESS: O=C(O)C1=NC=CC(O)=C1,cas:22468-26-4) is researched.Synthetic Route of C6H5NO3. The article 《Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952》 in relation to this compound, is published in Bioorganic & Medicinal Chemistry Letters. Let’s take a look at the latest research on this compound (cas:22468-26-4).

Optimization of novel azetidine compounds, which we had found as colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors, provided JTE-952 as a clin. candidate with high cellular activity (IC50 = 20 nM) and good pharmacokinetics profile. JTE-952 was also effective against a mouse collagen-induced model of arthritis (mouse CIA-model). Addnl., the x-ray co-crystal structure of JTE-952 with CSF-1R protein was shown to be a Type II inhibitor, and the kinase panel assay indicated that JTE-952 had high kinase selectivity.

The article 《Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952》 also mentions many details about this compound(22468-26-4)Category: chiral-catalyst, you can pay attention to it, because details determine success or failure

Reference:
Chiral Catalysts,
Chiral catalysts – SlideShare