455279-96-6Relevant articles and documents
Method for synthesizing 3-(4-methyl-1H-imidazole-1-yl)-5-(trifluoromethyl) aniline
-
Paragraph 0029-0031, (2020/10/14)
The invention relates to a method for synthesizing 3-(4-methyl-1H-imidazole-1-yl)-5-(trifluoromethyl) aniline, which comprises the following steps: 1, by using 3,5-diaminobenzotrifluoride as a raw material, carrying out protection to obtain a mono-substituted product and an intermediate byproduct; and 2, carrying out a cyclization reaction on the mono-substituted product, and carrying out deprotection to obtain the 3-(4-methyl-1H-imidazole-1-yl)-5-(trifluoromethyl) aniline. The synthesis process is safe and reliable, and has the advantages of low cost, easy control of reaction, simple post-treatment, economy, environmental protection and the like.
Isothiazoles as active-site inhibitors of HCV NS5B polymerase
Yan, Shunqi,Appleby, Todd,Gunic, Esmir,Shim, Jae Hoon,Tasu, Tania,Kim, Hongwoo,Rong, Frank,Chen, Huaming,Hamatake, Robert,Wu, Jim Z.,Hong, Zhi,Yao, Nanhua
, p. 28 - 33 (2007/10/03)
Isothiazole analogs were discovered as a novel class of active-site inhibitors of HCV NS5B polymerase. The best compound has an IC50 of 200 nM and EC50 of 100 nM, which is a significant improvement over the starting inhibitor (1). The X-ray complex structure of 1 with HCV NS5B was obtained at a resolution of 2.2 A, revealing that the inhibitor is covalently linked with Cys 366 of the 'primer-grip'. Furthermore, it makes considerable contacts with the C-terminus, β-loop, and more importantly, to the active-site of the enzyme. The uniqueness of this binding mode offers a new insight for the rational design of novel inhibitors for HCV NS5B polymerase.