84445-92-1Relevant academic research and scientific papers
Synthesis method of key raw material 2-chloro-6-methylaniline of dasatinib
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, (2021/04/21)
The invention discloses a synthetic method of a key raw material 2-chloro-6-methylaniline of dasatinib. The method comprises the following steps: firstly, protecting a 1-site amino group of 2-nitro-6-methylaniline, then reducing a 2-site nitro group of 2-nitro-6-methylaniline into an amino group, then carrying out diazotization reaction, carrying out chlorine substitution on the 2-site amino group by using cuprous chloride, and finally, carrying out acidolysis to remove a 1-site amino protecting group to obtain 2-chlorine-6-methylaniline. The method has the advantages of cheap and easily available raw materials, easily controllable reaction, simple operation steps, simple post-treatment, recyclable solvents, small pollution, and suitableness for large-scale production of generative enterprises.
Synthesis of N-Acetylbenzimidazole Derivatives
Tanaka, Kenjiro,Shimazaki, Michiko,Murakami, Yasuoki
, p. 2714 - 2722 (2007/10/02)
For the structure determination of thiazolobenzimidazol-3(2H)-one derivatives (2 or 3) they were converted to the corresponding 1-acetylbenzimidazoles (4) by desulfurization.The latter compounds (4) were alternatively prepared by the cyclization of 2-aminoacetanilide derivatives (5) with CS2 in dimethylformamide (DMF), followed by desulfurization with Raney Ni.However, the reactions of 5 with ethyl orthoformate/H2SO4 in DMF gave a mixture of 4 and its acetyl-rearranged product (7).Keywords-acetyl group; rearrangement; thiazolobenzimidazol-3(2H)-one; N-acetylbenzimidazoles; ethyl orthoformate; carbon disulfide; desulfurization
