Potassium Phosphate, Tribasic → (r/s)-3-(Tert-butoxycarbonylamino)-1-(4-cyclopropyl-5-isoquinolinesulfonyl)-pyrrolidine

Participants

Reaction Conditions

Reaction Steps

A suspension of Intermediate 1 (200 mg) obtained in Example 1, Step A, cyclopropylboronic acid (57 mg, Aldrich), anhydrous potassium phosphate (372 mg, Aldrich), and tricyclohexylphosphonium tetrafluoroborate (33 mg, Aldrich) in toluene (2 ml) is added with palladium acetate (10 mg, Wako Pure Chemical Industries), and the mixture is stirred at 80° C. with heating for 14 hours under a nitrogen gas atmosphere. The reaction mixture is cooled to room temperature, and then added with ethyl acetate (5 ml), and the insoluble matters are removed by filtration through Celite. The solvent is evaporated under reduced pressure, and the residue is purified by silica gel chromatography (n-hexane:ethyl acetate=1:1) to obtain the title compound (53 mg (predictive yield)).

Provenance & Evidence