Acetic Acid → (1S)-{1-(1h-indol-3-ylmethyl)-2-[5-(4-phenylaminomethyl-phenyl)-pyridin-3-yloxy]-ethyl}-carbamic acid tert-butyl ester

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Reaction Steps

A solution of Example 116A (0.03 g, 0.06 mmol) in 2 mL of MeOH was cooled to 0° C. then treated with aniline (0.018 g 0.2 mmol), NaBH3CN (0.004 g, 0.06 mmol) and AcOH (1 ml). The mixture was allowed to warm to room temperature overnight. The mixture was diluted with ethyl acetate (20 ml), washed with water (10 ml) and brine (10 ml). The ethyl acetate was evaporated off and the residue was used without further purification.

Provenance & Evidence