A novel and practical method for the synthesis of 3,5-bis(trifluoromethyl)-4,5-dihydro-1H-pyrazoles by [3+2] cycloaddition reactions of α-(trifluoromethyl)styrenes with 2,2,2-trifluorodiazoethane (CF3CHN2) has been d...A novel and practical method for the synthesis of 3,5-bis(trifluoromethyl)-4,5-dihydro-1H-pyrazoles by [3+2] cycloaddition reactions of α-(trifluoromethyl)styrenes with 2,2,2-trifluorodiazoethane (CF3CHN2) has been developed. The cyclization reaction proceeds smoothly in the presence of a catalytic amount of Et_(3)N, affording a variety of bis(trifluoromethyl)-substituted 2-pyrazolines in good to excellent yields. This method also exhibits a broad substrate scope and tolerates various functional groups.展开更多
基金support from the National Key Research and Development Program of China(No.2017YFD0200505)。
文摘A novel and practical method for the synthesis of 3,5-bis(trifluoromethyl)-4,5-dihydro-1H-pyrazoles by [3+2] cycloaddition reactions of α-(trifluoromethyl)styrenes with 2,2,2-trifluorodiazoethane (CF3CHN2) has been developed. The cyclization reaction proceeds smoothly in the presence of a catalytic amount of Et_(3)N, affording a variety of bis(trifluoromethyl)-substituted 2-pyrazolines in good to excellent yields. This method also exhibits a broad substrate scope and tolerates various functional groups.