Morpholine → 1-(4-Morpholin-4-yl-phenyl)-3-aza-bicyclo[3.1.0]hexane-3-carboxylic acid tert-butyl ester

Participants

Reaction Conditions

Reaction Steps

To a solution of 1-(4-bromo-phenyl)-3-aza-bicyclo[3.1.0]hexane-3-carboxylic acid tert-butyl ester (Intermediate I, 680 mg, 2.01 mmol) in anhydrous toluene (20 mL) were added Pd2(dba)3 (4.6 mg, 0.005 mmol), BINAP (9.4 mg, 0.015 mmol), sodium tert-butoxide (232 mg, 2.41 mmol) and morpholine (0.2 mL, 2.21 mmol) at r.t. and reaction mixture was stirred at 90° C. for 4 h. Reaction mixture was then concentrated and crude product was purified by column chromatography (silica gel, 1:9 EtOAc:Pet. ether) to afford the title compound as white solid (456 mg, 66%).

Provenance & Evidence