On July 21, 2011, Aronov, Alex; Come, Jon H.; Davies, Robert J.; Pierce, Albert C.; Wang, Jian; Nanthakumar, Suganthini; Cao, Jingrong; Bandarage, Upul K.; Krueger, Elaine; Tiran, Amaud Le; Liao, Yusheng; Messersmith, David; Collier, Philip N.; Grey, Ronald; O’Dowd, Hardwin; Henderson, James A.; Grillot, Anne-Laure published a patent.HPLC of Formula: 877149-10-5 The title of the patent was Preparation of dihydropyrrolopyridinone derivatives and analogs for use as phosphatidylinositol 3-kinase inhibitors. And the patent contained the following:
Title compounds I [A = N, CH, CCH3, or COCH3; B = N, CH, CF, etc.; or A=B is a S atom; C = N, CH, CCl, COH, etc.; D = N, CH, CCO2H, CCN, etc.; E = N, CH, CF, COH, etc.; provided no more than two A, B, C, D, or E is N; X = N or CH; Y = N, CH, or CCH3; R1 = (un)substituted Ph, heteroaryl, pyridone, fused bicyclic heteroaryl,or heterocyclic ring system; R2 = H, F, Cl, CF3, OCF3, etc.; R3 = H, (un)substituted aliphatic, cycloaliphatic, OH, etc.; R4 = H or alkyl; or R3 and R4 together with the carbon to which they are attached form an (un)substituted cycloaliphatic ring, heterocyclic ring containing up to two atoms selected from N or O, or alkenyl; with provisions], and their pharmaceutically acceptable salts, are prepared and disclosed as phosphatidylinositol 3-kinase (PI3K) inhibitors. Thus, e.g., II was prepared by chlorination of Et 2-methyl-6-oxo-1,6-dihydropyridine-3-carboxylate followed by coupling with 2,3-dimethoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine (preparation given), bromination, and cyclization with 2-(4-amino-1H-pyrazol-1-yl)acetonitrile. Select I were evaluated in PI3K-γ inhibition assays, e.g., II demonstrated a Ki value of less than 0.1 μM. The experimental process involved the reaction of Methyl 4-bromo-2-chloro-6-methylbenzoate(cas: 877149-10-5).HPLC of Formula: 877149-10-5
The Article related to pyridinone pyrrolo derivative preparation phosphatidylinositol kinase pi3k inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 877149-10-5
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