期刊
JOURNAL OF MOLECULAR STRUCTURE
卷 1120, 期 -, 页码 228-233出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.molstruc.2016.05.026
关键词
5-chloro-2-(2-methylpyrazolo[1,5-a]pyrimidin-5-yl)phenol; 5-chloro-2-(pyrazolo [1,5-a]pyrimidin-7-yl)phenol; Phytopathogens fungi; Antifungal activity
资金
- National Natural Science Foundation of China [21542002, 2015.01-2016.12]
Under microwave radiation, isomers 2-(pyrazolo[1,5-a]pyrimidin-5-yl)phenols (3) and 2-(pyrazolo[1,5-a]pyrimidin-7-yl)phenols (4) were simultaneously obtained by the condensation of chromones and 3-aminopyrazoles. These two isomers were fully characterized by IR, H-1 NMR, C-13 NMR and HRMS. In addition, a representative product 5-chloro-2-(2-methyl-pyrazolo[1,5-a]pyrimidin-5-yl)phenol (3e) was further conformed by the single crystal X-ray diffraction. The antifungal abilities of the obtained products 3 and 4 were evaluated against five phytopathogenic fungi (Cytospora sp., Colletotrichum gloeosporioides, Botrytis cinerea, Alternaria solani and Fusarium solani). The results revealed that 2-(pyrazolo[1,5-a]pyrimidin-5-yl)phenol (3a) and 4-chloro-2-(2-methylpyrazolo[1,5-a]pyrimidin-7-yl)phenol (4e) exhibited good antifungal abilities against Colletotrichum gloeosporioides with the IC50 values of 24.90 and 28.28 mu g/mL, respectively. (C) 2016 Published by Elsevier B.V.
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