Formaldehyde → HCID 86705583, compound

Participants

Reaction Steps

To a solution of 420 (0.35 g, 1.52 mmol) and MeOH (5 mL) was added HCHO (37% in water, 0.42 mL, 15.2 mmol). The mixture was stirred at RT for 2 h and then NaCNBH3 (1.43 g, 22.8 mmol) was added. The reaction was stirred at RT for 3 h. The reaction was quenched with aqueous NH4OH (50 mL) and the mixture was extracted with EtOAc (3×10 mL). The combined organic phases were washed with water (3×50 mL), dried (Na2SO4) and concentrated in vacuo to afford 0.830 g of cis-(±)-4-(4-chloro-3-fluorophenoxy)-1-methylpyrrolidin-3-ol as a brown oil (422) which used for next step without further purification: LC-MS (ESI) m/z 246 (M+H).

Provenance & Evidence