SYNTHESIS OF CHIRAL PIPERIDINE DERIVATIVES VIA ASYMMETRIC HECK REACTION
Chiral piperidine backbones are widely found in the drugs and bioactive natural products.In the present study,a new asymmetric Heck reaction has been developed that allows synthesis of chiral piperidine derivatives.After screening of reaction conditions,the optimal conditions were obtained:[Pd(allyl)Cl]2(5 mol%)as catalyst,L5(10 mol%)as ligand,NaOMe(3.0 equiv)as base,mixed solvent(PhMe/MeOH = 5/1)at 110℃for 20 hours.This method displays a good substrate scope,which could facilitate the preparation of chiral piperidine derivatives with quaternary stereogenic centers.
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维普
