On April 17, 2003, Kallander, Lara S.; Ryan, Dominic M.; Thompson, Scott K. published a patent.Reference of 4-(p-Tolyl)-1H-1,2,3-triazole The title of the patent was Preparation of 4-phenyl-1H-1,2,3-triazoles as inhibitors of type 2 methionine aminopeptidase (MetAP2). And the patent contained the following:
The title compounds [I; X, Y = N, CH, CR, provided that X and Y are not both CR; R = H, halo, alkyl, etc.; R1 = H, halo, alkyl, etc.; R2, R3 = H, halo, alkyl, etc.] which are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase, and useful in treating conditions mediated by angiogenesis, such as cancer, hemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity, were prepared Thus, reacting 3-ethynylphenylamine with Et glyoxalate in the presence of NaBH(OAc)3 and AcOH in 1,2-dichloroethane followed by treating the resulting ethoxycarbonylmethyl-(3-ethynylphenyl)amine with trimethylsilylazide in PhMe afforded I [X, Y = CH; R1, R2 = H; R3 = NHCH2CO2Et]. The compounds I show MetAP2 inhibitor activity having IC50 values in the range of 0.0001 to 100 μM. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).Reference of 4-(p-Tolyl)-1H-1,2,3-triazole
The Article related to phenyltriazole preparation methionine aminopeptidase metap2 inhibitor angiogenesis antitumor, triazole phenyl preparation methionine aminopeptidase metap2 inhibitor angiogenesis antitumor and other aspects.Reference of 4-(p-Tolyl)-1H-1,2,3-triazole
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics