87-63-8Relevant articles and documents
Synthesis method of key raw material 2-chloro-6-methylaniline of dasatinib
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Paragraph 0016; 0033; 0037-0038; 0042, (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.
Preparation method of 2-chloro-6-methylaniline
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Paragraph 0030-0040, (2021/02/13)
The invention discloses a preparation method of 2-chloro-6-methylaniline. The method comprises the following steps: by using 3-chloro-5-methyl-4-nitroaniline as a starting raw material, water as a solvent and sulfuric acid as a reactant, carrying out diazotization reaction to eliminate amino groups, carrying out hypophosphorous acid reduction to obtain an intermediate, and finally, carrying out nitro reduction by using iron powder, and preparing 2-chloro-6-methylaniline through a one-pot reaction. The method has the advantages of short reaction steps, mild reaction conditions, high product yield and low cost, and provides a universal new method for preparing the 2-chloro-6-methylaniline.
Highly selective hydrogenation of halogenated nitroarenes over Ru/CN nanocomposites by: In situ pyrolysis
Yue, Shengnan,Wang, Xueguang,Li, Shaoting,Sheng, Yao,Zou, Xiujing,Lu, Xionggang,Zhang, Chunlei
, p. 11861 - 11869 (2020/07/28)
A highly chemoselective and recyclable ruthenium catalyst for the hydrogenation of halogenated nitroarenes has been prepared via the simple in situ calcination of a mixture of melamine, glucose and ruthenium trichloride. Superfine Ru particles (2.3 ± 0.3 nm) were obtained and highly dispersed in the nitrogen-doped carbon matrix. The Ru/CN catalyst smoothly transforms a variety of halogenated nitroarenes to the corresponding haloanilines with high intrinsic activity (e.g. TOF = 1333 h-1 for p-chloronitrobenzene) and selectivity of more than 99.6percent. Furthermore, through an analysis of the products in the reaction process, it was concluded that there are two parallel reaction pathways (a direct pathway and an indirect pathway) for the hydrogenation of aromatic nitro compounds over the Ru/CN catalyst, and the direct pathway was proved to be dominant in catalyzing the intermediates. This journal is