Methylamine → t-Butyl 2-(2-(4-fluoro-3-(methylsulfonyl)phenyl)-4-((methylamino)methyl)phenoxy)acetate

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Reaction Steps

Intermediate 29 (270 mg, 0.66 mmol, 1 eq) was stirred with methylamine (1.5 mL of a 0.88 M THF solution, 1.32 mmol, 2 eq.) in MeOH for 2 h. Sodium borohydride (50 mg, 0.66 mmol, 1 eq.) was added, and the resulting mixture was stirred at room temperature for an additional 2 h. Water (3 mL) was added and the MeOH was removed in vacuo. The resulting solution was extracted with EtOAc, dried (Na2SO4), and concentrated in vacuo to give 260 mg (93%) of t-butyl 2-(2-(4-fluoro-3-(methylsulfonyl)phenyl)-4-((methylamino)methyl)phenoxy)acetate (30) as oil.

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