文献类型：专利

英文题名：Preparation of 2-substituted benzoxazole compound, involves catalytically reacting benzylamine, benzyl alcohol or benzaldehyde compound, and o-aniline compound, extracting, concentrating, drying, and carrying out column chromatography

作者：LIU R;LIU Y;LIAO N;JIN X

机构：[1]UNIV EAST CHINA SCI & TECHNOLOGY

申请号：CN103102321-A

申请日：2013-01-21

公开日：2013-05-15

语种：英文

收录：DERWENT

摘要：NOVELTY - A benzylamine compound or benzyl alcohol compound (I), or benzaldehyde compound (II), and o-aniline compound (III) are mixed with a catalyst and a solvent, and reacted at 110-150 degrees C for 20-45 hours. After reaction completion, the catalyst is separated. Water and ethyl acetate are added, and extraction is carried out. The organic phases are combined, concentrated, and dried with anhydrous sodium sulfate. 2-Substituted benzoxazole compound (IV) is then obtained by column chromatography. USE - Preparation of 2-substituted benzoxazole compound (claimed). ADVANTAGE - The method does not require the usage of oxidant and hydrogen acceptor, enables recycling of used partial catalysts, and is high in atom economy, simple in post-treatment, and mild in reaction conditions. DETAILED DESCRIPTION - A benzylamine compound or benzyl alcohol compound of formula (I) or a benzaldehyde compound of formula (II), and o-aniline compound of formula (III) are used as raw materials. Metal palladium, platinum or ruthenium is used as catalyst. N,N-Dimethylformamide, N,N-dimethylacetamide or N-methylpyrrolidone is used as solvent. The raw materials are mixed with the catalyst and solvent. The molar ratio of raw materials, catalyst, and solvent is 1:1:0.01-0.1. The mixture is chemically reacted at 110-150 degrees C for 20-45 hours. After reaction completion, the catalyst is separated. Water and ethyl acetate are added, and extraction is carried out to obtain water phase and organic phase. The organic phases are combined, concentrated, and dried with anhydrous sodium sulfate. 2-Substituted benzoxazole compound of formula (IV) is then obtained by column chromatography. R1,R2=H, Me, OMe, Cl, NO2, F or t-Bu; X1=NH or O;and X2=NMe, O or S.