Synthesis of N~2-arylaminopyrimidine-5-carbonitrile derivatives via S_NAr amination reaction

• 作 者: Shahnaz Rostamizadeh Masoomeh Nojavan Reza Aryan
• 机 构: Department of Chemistry,Faculty of Science,K.N.Toosi University of Technology,Department of Chemistr
• 出 处: Chinese Chemical Letters
• 发表日期: 2015年01期
• 关键词: pyrimidine amination carbonate substituent replaced reagent starting facile yiel

An efficient and high-yielding synthesis of N~2-arylaminopyrimidine-5-carbonitrile derivatives starting from arylamines and 2-methylthio-pyrimidine-5-carbonitriIe derivatives has been developed in the presence of cesium carbonate as basic reagent.This new protocol showed high chemical tolerance for a range of functional groups,and only the methylthio substituent on C2 of the pyrimidine ring was replaced with arylamine derivatives under the reaction conditions.

An efficient and high-yielding synthesis of N ~ 2-arylaminopyrimidine-5-carbonitrile derivatives starting from arylamines and 2-methylthio-pyrimidine-5-carbonitriIe derivatives has been developed in the presence of cesium carbonate as basic reagent. This new protocol showed high chemical tolerance for a range of functional groups, and only the methylthio substituent on C2 of the pyrimidine ring was replaced with arylamine derivatives under the reaction conditions.