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With N-ethyl-N,N-diisopropylamine In 1,4-dioxane; water for 7h; Reflux; Inert atmosphere;
7
A suspension of Compound 4 ( 70 mg, 196 μmol ), potassium 5-chloro-2- thiophenetrifluoroborate ( 88 mg, 392 μmol ), dichlorobis(triphenylphosphine)palladium ( 16 mg, 19.6 μmol ) and diisopropylethylamine ( 103 μL, 589 μmol ) in dioxane/water (10 : 1, 2 mL) was refluxed for 4 hours under argon atmosphere. After cooling, potassium 5-chloro-2- thiophenetrifluoroborate ( 88 mg, 392 μmol ), dichlorobis(triphenylphosphine)palladium ( 16 mg, 19.6 μmol ) and diisopropylethylamine ( 103 μL, 589 μmol ) were added thereto and the mixture was refluxed for 3 hours under argon atmosphere. After cooling, the reaction mixture was diluted with ethyl acetate, filtered through Chem Elut ( Varian Inc. ) and Bond Elut ( Varian Inc. ), and concentrated under reduced pressure. The residue was purified by silica gel column chromatography ( hexane -> hexane : ethyl acetate = 23 : 2 ) to give Compound 5 ( 39 mg, 45 % ) as a powder.
(R)-4-(5-chlorothiophen-2-yl)-4-(1H-indol-3-yl)butan-2-one[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
93%
With (R)-3,3’-bis(2,3,5,6-tetrafluoro-4-(trifluoromethyl)phenyl)-1,1’-binaphthyl-2,2’-diol In toluene at 80℃; for 6.5h; Molecular sieve; Inert atmosphere; Sealed tube; enantioselective reaction;
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