| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 5213080 | Tetrahedron | 2016 | 10 Pages |
Abstract
A convenient and robust stereocontrolled procedure has been developed for the synthesis of novel trifluoromethyl-containing piperidine and azepane β-amino ester stereoisomers. The synthesis started from readily available unsaturated bicyclic β-lactams and was based on oxidative cleavage of the ring CC double bond followed by ring closure of the diformyl intermediates in the presence of 2,2,2-trifluoroethylamine hydrochloride through reductive amination. The synthetic procedure has efficiently been extended towards the synthesis of mono- and difluorinated analogs.
Graphical abstractDownload high-res image (184KB)Download full-size image
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Renáta Anita Ábrahámi, Loránd Kiss, Pablo Barrio, Ferenc Fülöp,