On January 15, 2015, Hu, Shaojing; Liu, Xiangyong; Bai, Jinlong; Long, Wei published a patent.COA of Formula: C9H10N2O The title of the patent was Preparation of pyrimidines as protein tyrosine kinase modulators. And the patent contained the following:
Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative,and methods of treatment for diseases associated with protein kinase enzymic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed. Compounds I [X = absent, O, S, or NR16; R16 = H or alkyl; Y = halogen, OH, NH2, CN, N3, NO2, or (un)substituted alkyl; Z = O, S, NR20, or CR20R21; and each R20 or R21 independently = H, halogen, (un)substituted alkyl, or alkoxy; R1 = hydroxy, alkyl, haloalkyl, aryl, arylalkyl, etc.; R2 = H, F, or alkyl; or R3 = H, halogen, or a 5 or 6 member heterocyclic ring; R4 = H, alkoxy, alkenyloxy, cycloalkyloxy, halogen, etc.; R5 = H, F, alkyl, haloalkyl, alkoxy, etc.; R6 = H, halo, CN, NO2, cycloalkyl, etc.; R7 = H, halo, alkyl, alkoxy, alkenyloxy, etc.], and their pharmaceutically acceptable salts, are prepared and disclosed. Thus, e.g., II was prepared by. Compound II showed IC50 value of 27.9 nM in ALK assay, 44.3 nM in EGFR (ErB1) L858R assay and 4.08 nM in EGFR (ErbB1) T790M L858R assay. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).COA of Formula: C9H10N2O
The Article related to pyrimidine preparation protein tyrosine kinase, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C9H10N2O
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics