1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine) → 4-(2-Cyano-4-methoxy-phenyl)-piperazine-1-carboxylic acid tert-butyl ester

Participants

Reaction Conditions

Reaction Steps

A mixture of Boc-homopiperazine (483 mg, 2.59 mmol), 2-bromo-5-methoxybenzonitrile (500 mg, 2.36 mmol), Pd2(dba)3 (108 mg, 0.12 mmol), xantphos (205 mg, 0.35 mmol), sodium t-butoxide (666 mg, 7.08 mmol) in degassed anhydrous dioxane (10 mL) was heated at 90° C. for 2 h. The mixture was allowed to cool and filtered through celite. The filtrate was concentrated and purified by chromatography (EtOAc/hexanes) to yield the title compound (691 mg, 92%). m/z (M+1) 318.39.

Provenance & Evidence