反应详情

温度

75 °C

1-Tert-butoxycarbonyl-4-1H-pyrazoleboronic acid pinacol ester (126 mg), Tris(dibenzylideneacetone)dipalladium(0) [Pd2(dba)3 (7 mg)], K3PO4 (185 mg) and 2-dicyclohexylphosphinno-2′,6′-dimethoxybiphenyl (12 mg) are added to a solution of 3-(4-bromo-naphthalen-1-yl)-5-(3,5-dichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazole (140 mg) in dry toluene (2.4 ml). After 16 hours at 75° C. the reaction is cooled down to room temperature and filtrated. The filtrate is concentrated in vacuo. The crude product is purified on a semi-preparative HPLC to yield 4-{4-[5-(3,5-dichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-naphthalen-1-yl}-pyrazole-1-carboxylic acid tert-butyl ester (compound 1.10, Table 1) as a colorless oil.

1. filtrationfiltrated
2. concentrationThe filtrate is concentrated in vacuo
3. customThe crude product is purified on a semi-preparative HPLC