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Synthesis of silicon-containing azole derivatives with magnesium bromide diethyl etherate,and an investigation of their fungicidal activities |
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| Authors: | Itoh Hiroyuki Kajino Hisaki Tsukiyama Takahiro Tobitsuka Junzo Ohta Hiroshi Takahi Yukiyoshi Tsuda Mikio Takeshiba Hideo |
| Affiliation: | a Agroscience Research Laboratories, Sankyo Co., Ltd., Yasu, 1041, Yasu, Yasu-cho, Yasu-gun, Shiga-ken, 520-2342, Japan b Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., 2-58, Hiromachi, 1-chome, Shinagawa-ku, Tokyo, 140-8710, Japan |
| Abstract: | Enhancement of magnesium bromide diethyl etherate in addition reaction of trimethylsilylmethylmagnesium chloride 5 to 2-(1H-1,2,4-triazol-1-yl)acetophenones 6 allowed us to prepare silicon-containing azole derivatives, which were tested for fungicidal activity and phytotoxicity. Among them, 2-(4-fluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-3-trimethylsilylpropan-2-ol 1a was determined to be the most effective and potential candidate for novel fungicide. |
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