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One‐step synthesis of 2,4,5‐trisubstituted pyrimidines

Zhang Chuang-junKey Laboratory of the Ministry of Education for Medicinal Resources and Natural Pharmaceutical Chemistry, National Engineering Laboratory for Resource Development of Endangered Crude Drugs in Northwest of China, and School of Chemistry and Materials Science, Shaanxi Normal University, Xi'an 710062, People's Republic of ChinaWen‐Yong HanKey Laboratory of the Ministry of Education for Medicinal Resources and Natural Pharmaceutical Chemistry, National Engineering Laboratory for Resource Development of Endangered Crude Drugs in Northwest of China, and School of Chemistry and Materials Science, Shaanxi Normal University, Xi'an 710062, People's Republic of ChinaMi‐Xiang GaoKey Laboratory of the Ministry of Education for Medicinal Resources and Natural Pharmaceutical Chemistry, National Engineering Laboratory for Resource Development of Endangered Crude Drugs in Northwest of China, and School of Chemistry and Materials Science, Shaanxi Normal University, Xi'an 710062, People's Republic of ChinaFei‐Fei XuKey Laboratory of the Ministry of Education for Medicinal Resources and Natural Pharmaceutical Chemistry, National Engineering Laboratory for Resource Development of Endangered Crude Drugs in Northwest of China, and School of Chemistry and Materials Science, Shaanxi Normal University, Xi'an 710062, People's Republic of ChinaZun‐Ting ZhangKey Laboratory of the Ministry of Education for Medicinal Resources and Natural Pharmaceutical Chemistry, National Engineering Laboratory for Resource Development of Endangered Crude Drugs in Northwest of China, and School of Chemistry and Materials Science, Shaanxi Normal University, Xi'an 710062, People's Republic of China
2011en
ABI

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Abstract A simple and straightforward methodology towards the synthesis of 2,4,5‐trisubstituted pyrimidines has been developed by one‐step reaction of isoflavones with thiourea or guanidine. Ten 2‐mercapto‐4,5‐diphenylpyrimidines and eight 2‐amino‐4,5‐diphenylpyrimidines were reported. All of them were characterized by FT‐IR, NMR, and elemental analysis. A variety of substrates can participate in the process with good yields and high purities, making this methodology suitable for library synthesis in drug discovery. J. Heterocyclic Chem., (2011).

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