Tricyclohexylphosphine → 2-Cyclopropyl-4-{2,2,2-trifluoro-1-[4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-yl]-ethoxymethyl}-benzonitrile

温度

10 °C

147 mg 2-Bromo-4-{2,2,2-trifluoro-1-[4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-yl]-ethoxymethyl}-benzonitrile, 15 mg Tricyclohexylphosphine, 71 mg Cyclopropylboronic acid and 224 mg Tripotassiumphosphate monohydrate were dissolved in a mixture of 2 ml toluene and 0.2 ml water. The reaction mixture was degassed and 62 mg palladium(II) acetate were added and the reaction mixture heated under microwave irradiation at 10° C. for 2.5 hours. The cooled reaction mixture was diluted by addition of 50 ml ethyl acetate and filtered. The filtrate was evaporated and the residue purified by reverse phase HPLC to obtain 97 mg 2-Cyclopropyl-4-{2,2,2-trifluoro-1-[4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-yl]-ethoxymethyl}-benzonitrile as an oil.

1. customThe reaction mixture was degassed
2. addition62 mg palladium(II) acetate were added
3. customThe cooled reaction mixture
4. filtrationfiltered
5. customThe filtrate was evaporated
6. customthe residue purified by reverse phase HPLC

ORDレコード

ord-10bb620c473547968ea0bd0bd254c052

出典データセット

uspto-grants-2010_11

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US07834030B2