Published December 14, 2016 | Version Supplemental Material
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Diastereoselective access to substituted 4-aminopiperidines via a pyridine reduction approach

  • 1. ROR icon Pfizer (United States)
  • 2. ROR icon California Institute of Technology

Abstract

We describe herein a diastereoselective approach to access substituted-4-aminopiperidines from pyridine precursors. This methodology has successfully been applied to synthesize 2-alkyl substrates as well as more complex molecular entities of interest to the pharmaceutical industry.

Additional Information

© 2016 Elsevier. Received 11 October 2016; revised 21 October 2016; accepted 27 October 2016; available online 2 November 2016. The authors would like to thank Jason Ewanicki and Wei Wang for stereochemical analysis of 2, 5, 15, and 18; Phuong Tran for purification of 5 via liquid chromatography; and Loanne Chung for separation of cis/trans diastereomers of 2 via liquid chromatography. Additionally, the authors would like to thank Ted W. Johnson and Robert Kania for help in preparing this manuscript.

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Additional details

Identifiers

Eprint ID
73185
DOI
10.1016/j.tetlet.2016.10.107
Resolver ID
CaltechAUTHORS:20170103-150357846

Dates

Created
2017-01-04
Created from EPrint's datestamp field
Updated
2021-11-11
Created from EPrint's last_modified field