On July 3, 2008, Berdini, Valerio; Besong, Gilbert Ebai; Callaghan, Owen; Carr, Maria Grazia; Congreve, Miles Stuart; Gill, Adrian Liam; Griffiths-Jones, Charlotte Mary; Madin, Andrew; Murray, Christopher William; Nijjar, Rajdeep Kaur; O’Brien, Michael Alistair; Pike, Andrew; Saxty, Gordon; Taylor, Richard David; Vickerstaffe, Emma published a patent.Product Details of 1036991-35-1 The title of the patent was Preparation of bicyclic heterocyclic compounds as FGFR inhibitors. And the patent contained the following:
The title compounds I [X1, X2, X3 = C or N, such that at least one of X1-X3 = N; X4 = CR3 or N; X5 = CR5, N or C(O); provided that no more than 3 of X1-X5 = N; R1 = NHCONR4R5, NHCO2R4, NHCSOR4, etc.; R3 = halo, H, alkyl, etc.; R3 = H, halo, alkyl, etc.; R4, R5 = H, alkyl, cycloalkyl, etc.; A = (un)substituted (non)aromatic carbocyclic or heterocyclic group; with the provisos], useful in the treatment of diseases, e.g. cancer, were prepared E.g., a 2-step synthesis of II, starting from 6-chloro-3-iodoimidazo[1,2-a]pyridine with 3-acetylaminophenylboronic acid, was given. Exemplified compounds I were tested in in vitro FGFR3 and PDGFR kinase assays. Many compounds I showed IC50 of <10 渭M or provided at least 50% inhibition of the FGFR3 activity at a concentrate of 10 渭M. Preferred I showed IC50 of <1 渭M or provided at least 50% inhibition of the FGFR3 activity at a concentrate of 1 渭M. Pharmaceutical composition comprising the compound I is disclosed. The experimental process involved the reaction of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile(cas: 1036991-35-1).Product Details of 1036991-35-1
The Article related to bicyclic heterocyclic imidazopyridine preparation fibroblast growth factor receptor inhibitor, fgfr3 inhibitor antitumor bicyclic heterocyclic imidazopyridine preparation and other aspects.Product Details of 1036991-35-1
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts