On December 1, 2011, Yang, Shengyong; Wei, Yuquan published a patent.Recommanded Product: 16230-24-3 The title of the patent was (Arylamino)purine derivatives as EGFR and VEGFR inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:
(Arylamino)purine derivatives of formula I and their preparation methods are disclosed. The derivatives of formula I have inhibitory effects on non-small cell lung cancer with deletion mutation of exon 19 or L858R point mutation of exon 21 in epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR). Compounds of formula I wherein R1 is H, C0-4 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-8 alkyl, C1-8 alkyl-C3-7 cycloalkyl, 3- to 8-membered heterocycloalkyl, 3- to 8-membered heterocycloalkylamino and 6- to 8-membered (hetero)aryl; R2 is H, NH2, OH, F, Cl, Br, CF3, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylamino, 6- to 12-membered aryloxy and 6- to 12-membered arylamino; R3 is C3-7 cycloalkyl, C1-8 alkyl-C3-7 cycloalkyl and 6- to 80-membered (hetero)aryl; R4-R8 are independently H, F, Cl, Br, CF3, C1-8 alkoxy, C0-4 dioxaalkylene, (1-methyl-4-piperidinyl)aminocarbonyl, (1-methyl-4-piperazinyl)aminocarbonyl, etc.; are claimed. Example compound I (R1 = Pr-i, R2 = R5 = R6 = R7 = R8 = H, R3 = 4-bromphenyl and R4 = 4-methyl-1-piperazinyl) was prepared via cyclocondensation of 5-amino-4-(isopropylamino)-2-[4-(4-methylpiperazin-1-yl)phenyl]aminopyrimidine with 4-bromophenyl isothiocyanate. All the invention compounds were evaluated for their EGFR and VEGFR inhibitory activity. From the assay, it was determined that example compound I exhibited the IC50 values of 0.001 and 0.004 μM against RGFR-L858R and VEGFR2, resp. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Recommanded Product: 16230-24-3
The Article related to arylamino purine preparation egfr vegfr inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 16230-24-3
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics