A facile synthesis and fungicidal activities of novel fluorine-containing pyrido[4,3-d]pyrimidin-4(3H)-ones |
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Authors: | Qingyun Ren Hongwu He Yucheng Gu |
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Affiliation: | a The Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, 152 Luoyu Road, Wuhan, Hubei 430079, PR China b Jealott's Hill International Research Centre, Syngenta, Bracknell, Berkshire RG42 6EY, United Kingdom |
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Abstract: | Sixteen novel 2-substituted-5,8,9-trimethyl-3-(4-fluoro-substituted)phenyl-thieno[3′,2′-5,6] pyrido[4,3-d]pyrimidin-4(3H)-ones 5a-5p were designed and have been successfully synthesized via tandem aza-Wittig and annulation reactions of the corresponding iminophosphorances 1, para-fluoro phenyl isocyanate, and substituted phenols or amines in 73-90% isolated yields. Their structures were clearly verified by IR, 1H NMR, EI-MS spectroscopy and elemental analysis, and in the case of compound 5a, analyzed by single-crystal X-ray diffraction further. The results of preliminary bioassay indicated that some compounds possess inhibition activities against Rhizoctonia solani and Botrytis cinereapers at a dosage of 50 mg/L. |
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Keywords: | Pyrido[4,3-d]pyrimidin-4(3H)-one aza-Wittig reaction Synthesis Fungicidal activity |
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