Abstract

We reported the synthesis of (S)-pregabalin in a five-step sequence with 20% overall

yield. As a modification of the previously developed route, a Michael addition
between CH3NO2 and chiral oxaoxazolidinone was employed as a key operation for
introducing the methyleneamino group, which allowed avoiding the use of toxic
cyanide reagent and led to enantiomerically pure product (>99% ee) after the
recrystallization in appropriate solvent.

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information
Funding

This work was financially supported by the National Science and Technology Major
Project [No. 2018ZX09711002-002-009], the National Natural Science Foundation of
China [No. 81703358], and Science and Technology Commission of Shanghai Municipality
[Nos. 17431903900, 18QB1404200].