1-METHANESULFONYL-PIPERIDINE-3-CARBOXYLIC ACID ETHYL ESTER synthesis

Yield:-

Reaction Conditions:

in dichloromethane at 20; for 5 h;Cooling with ice;

Steps:

A representative procedure of N-substituted piperidine is as follows

General procedure: A solution of sulfonyl chloride (11.0 mmol) in DCM (10 mL) was added to a stirred solution of compound 10 (10.0 mmol) in DCM (20 mL) at ice bath. The reaction mixture was stirred at rt for 5 h. The reaction mixture was concen trated under reduced pressure. The residue was extracted with EtOAc (3 x 50 mL). The combined organic layers were washed with brine, dried, filtered and evaporated to afford crude product under reduced pressure. Purification on silica gel (hexanes/EtOAc = 8/1~4/1) afforded the following compound.

References:

Chang, Meng-Yang;Lin, Chung-Han;Lee, Tein-Wei [Tetrahedron Letters,2012,vol. 53,# 6,p. 627 - 631] Location in patent:supporting information; experimental part