- Method for synthesizing 3-(4-methyl-1H-imidazole-1-yl)-5-(trifluoromethyl) aniline
-
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.
- -
-
Paragraph 0029-0031
(2020/10/14)
-
- CYCLOPROPANECARBOXAMIDO-SUBSTITUTE AROMATIC COMPOUNDS AS ANTI-TUMOR AGENTS
-
Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.
- -
-
Paragraph 0242; 0243
(2015/07/22)
-
- Isothiazoles as active-site inhibitors of HCV NS5B polymerase
-
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.
- 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
-
-