Method for synthesizing 2-cyano-5-aryl-1H-imidazole compound

• Main Authors: YANG CUIFENG, WANG WEI, SONG PEIDONG, XU ZEGANG, ZHENG XIAORUI, RONG HAOJIE, CHEN TAO
• Format: Patent
• Language: Chinese; English
• Published: 25.11.2022
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a method for synthesizing a 2-cyano-5-aryl-1H-imidazole compound, which comprises the following steps: firstly, carrying out ring closing on alpha-halogen aryl ethanone and thiomethylisourea sulfate under the action of an acid-binding agent to synthesize the 2-thiomethyl-5-aryl-1H-imidazole compound; and then carrying out a reaction of substituting thiomethyl with cyano groups to obtain the 2-cyano-5-aryl-1H-imidazole compound. The reaction conditions are mild, and the phenomenon of severe temperature rise is avoided; the preparation steps are short, the 2-cyano-5-aryl-1H-imidazole compound is synthesized through two-step reaction, and the total yield of the two-step reaction is 54.9%. 本发明公开了一种合成2-氰基-5-芳基-1H-咪唑类化合物的方法，该方法首先将α-卤素芳基乙酮和硫甲基异脲硫酸盐，在缚酸剂的作用下合环合成2-硫甲基-5-芳基-1H-咪唑类化合物，然后经氰基取代硫甲基反应得到2-氰基-5-芳基-1H-咪唑类化合物。本发明反应条件温和，无剧烈升温现象发生；制备步骤短，经过两步反应就合成了2-氰基-5-芳基-1H-咪唑类化合物，两步反应总收率54.9％。