title: Synthesis of silicon-containing azole derivatives with magnesium bromide diethyl etherate, and an investigation of their fungicidal activities.
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.
authors.affiliation: Agroscience Research Laboratories, Sankyo Co., Ltd., Yasu, 1041, Yasu, Yasu-cho, Yasu-gun, Shiga-ken, Japan. hiroit@yasu.sankyo.co.jp
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Itoh
authors.forename: Hisaki
authors.initials: H
authors.lastname: Kajino
authors.forename: Takahiro
authors.initials: T
authors.lastname: Tsukiyama
authors.forename: Junzo
authors.initials: J
authors.lastname: Tobitsuka
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Ohta
authors.forename: Yukiyoshi
authors.initials: Y
authors.lastname: Takahi
authors.forename: Mikio
authors.initials: M
authors.lastname: Tsuda
authors.forename: Hideo
authors.initials: H
authors.lastname: Takeshiba
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001393:Azoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D004986:Ether / Q000737:chemistry; D005516:Food Microbiology; D005658:Fungi / Q000187:drug effects; D005659:Fungicides, Industrial / Q000138:chemical synthesis / Q000494:pharmacology; D007202:Indicators and Reagents; D009942:Organometallic Compounds / Q000737:chemistry; D010935:Plant Diseases / Q000382:microbiology; D017655:Silicon Compounds; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D001393:Azoles; D005659:Fungicides, Industrial; D007202:Indicators and Reagents; D009942:Organometallic Compounds; D017655:Silicon Compounds; D004986:Ether