Sodium borohydride → 6-tert-Butyl-2-(4-chloro-3-(hydroxymethyl)pyridin-2-yl)-8-fluorophthalazin-1(2H)-one

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Reaction Steps

To a solution of 2-(6-tert-butyl-8-fluoro-1-oxophthalazin-2(1H)-yl)-4-chloronicotinaldehyde 103b (2.0 g, 5.5 mmol) in methanol (30 mL) was added NaBH4 (700 mg, 16.5 mmol) at room temperature. The reaction mixture was stirred for 1 h and quenched with water (30 mL). It was then concentrated under reduced pressure and the residue was extracted with dichloromethane (3×30 mL). The combined organic phase was dried over anhydrous Na2SO4, filtered, and evaporated under reduced pressure to afford 116a as a white solid (1.8 g, 90%). MS: [M+H]+ 362.3.

Provenance & Evidence