Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases was written by Erra, Montse;Taltavull, Joan;Greco, Angelique;Bernal, Francisco Javier;Caturla, Juan Francisco;Gracia, Jordi;Dominguez, Maria;Sabate, Mar;Paris, Stephane;Soria, Salome;Hernandez, Begona;Armengol, Clara;Cabedo, Judit;Bravo, Monica;Calama, Elena;Miralpeix, Montserrat;Lehner, Martin D.. And the article was included in ACS Medicinal Chemistry Letters in 2017.Synthetic Route of C5H3ClN4 This article mentions the following:
The delta isoform of the phosphatidylinositol 3-kinase (PI3Kδ) has been shown to have an essential role in specific immune cell functions and thus represents a potential therapeutic target for autoimmune and inflammatory diseases. Herein, the optimization of a series of pyrrolotriazinones as potent and selective PI3Kδ inhibitors is described. The main challenge of the optimization process was to identify an orally available compound with a good pharmacokinetic profile in preclin. species that predicted a suitable dosing regimen in humans. Structure-activity relationships and structure-property relationships are discussed. This medicinal chem. exercise led to the identification of LAS191954 as a candidate for clin. development. In the experiment, the researchers used many compounds, for example, 4-Amino-6-chloropyrimidine-5-carbonitrile (cas: 60025-09-4Synthetic Route of C5H3ClN4).
4-Amino-6-chloropyrimidine-5-carbonitrile (cas: 60025-09-4) belongs to nitriles. Nitrile compounds can be prepared by the incorporation of a cyanide source through C–C bond formation or by dehydration of primary carboxamides. Nitrile groups in organic compounds can undergo a variety of reactions depending on the reactants or conditions. A nitrile group can be hydrolyzed, reduced, or ejected from a molecule as a cyanide ion.Synthetic Route of C5H3ClN4
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts