(+/-)-TRANS-4-(4-CHLOROPHENYL)PYRROLIDINE-3-CARBOXYLIC ACID HYDROCHLORIDE synthesis

Yield:-

Reaction Conditions:

with hydrogenchloride in water;1,2-dichloro-ethane at 20;

Steps:

17.A Step A:
(3S,4R)-1-BOC-4-(4-chlorophenyl)pyrrolidine-3-carboxylic acid (0.70 g, 2.15 mmol) obtained in Preparation 14 was dissolved in DCE (3 ml) and 4N HCl (3 ml) was added dropwise, and stirred at room temperature for 2 hours. MeOH (5 ml) was added to the reaction solution. Then, the reaction solution was stirred at room temperature for 3 hours and concentrated in vacuo. DCE (2 ml) and EtOAc (10 ml) were added to the obtained residue. Then, the reaction mixture was stirred at room temperature for 1 hour and filtered to give the title compound (0.46 g, 90.0%).MS[M+1]=240 (M+1)

References:

LG LIFE SCIENCE LTD. US2010/120783, 2010, A1 Location in patent:Page/Page column 12