Morpholine → HCID 69292803, compound

Participants

Reaction Conditions

Reaction Steps

To a suspension of 1.0 mg (0.0045 mmol) palladium(II) acetate, 4.06 mg (0.0065 mmol) 2,2′-bis-(diphenylphosphino)-1,1′-binaphtyl (BINAP) and 125 mg (0.384 mmol) cesium carbonate in 1 ml dry toluene, 100 mg (0.272 mmol) (R)-5-[1-(4-Bromo-phenyl)-ethylcarbamoyl]-thiophene-2-carboxylic acid methyl ester (see example 1, step 1) and 30.0 mg (0.344 mmol) morpholine were added under an argon atmosphere. The mixture was heated in the microwave oven (Emrys Optimizer) at 160° C. for 15 min. After cooling to room temperature, the reaction mixture was filtered and the solid was washed with toluene. The solvent of the combined filtrates was evaporated and the crude product purified by preparative HPLC to yield 7.9 mg (0.021 mmol) (R)-5-[1-(4-Morpholin-4-yl-phenyl)-ethylcarbamoyl]-thiophene-2-carboxylic acid methyl ester.

Provenance & Evidence