1,2-Dichloroethane → 3-(3,4-Difluorophenyl)-3-methoxypyrrolidine

Participants

Reaction Steps

Preparation according to Example 1. (+)-1-benzyl-3-(3,4-difluorophenyl)-3-methoxypyrrolidine (0.202 g, 0.66 mmol), 1,2-dichloroethane (20 ml), 1-chloroethyl chloroformate (0.38 g, 2.66 mmol) refluxed for 1 h, and methanol (20 ml) reflux 1 h Purification by HPLC on waters OBD C18, 5 μm (MeOH/33 mM NH3, 20:80 to 50:50) gave the title compound (0.111 g, 78%). [a]D=+5.8° (methanol). MS m/z (rel. intensity, 70 eV) 213 (M+, 1), 198 (44), 183 (84), 171 (bp), 141 (45).

Provenance & Evidence