1-Chloroethyl chloroformate → 3-(3-Chloro-5-fluorophenyl)-3-methoxypyrrolidine

Participants

Reaction Steps

Preparation according to Example 1: (+)-1-benzyl-3-(3-chloro-5-fluorophenyl)-3-methoxypyrrolidine (0.212 g, 0.66 mmol), 1,2-dichloroethane (20 ml), 1-chloroethyl chloroformate (0.38 g, 2.65 mmol). Purification by HPLC on waters OBD C18, 5 μm (MeOH/33 mM NH3, 20:80 to 50:50) gave the title compound 0.042 g (27%). [a]D=+2.7° (methanol). MS m/z (relative intensity, 70 eV) 229 (M+, 1), 214 (58), 199 (bp), 187 (75), 157 (37).

Provenance & Evidence