Synlett 2014; 25(20): 2891-2894
DOI: 10.1055/s-0034-1379481
letter
© Georg Thieme Verlag Stuttgart · New York

Chemoselective Zinc/HCl Reduction of Halogenated β-Nitrostyrenes: Synthesis of Halogenated Dopamine Analogues

Justin J. Maresh*
,
Arthur A. Ralko
,
Tom E. Speltz
,
James L. Burke
,
Casey M. Murphy
,
Zachary Gaskell
,
JoAnn K. Girel
,
Erin Terranova
,
Conrad Richtscheidt
,
Mark Krzeszowiec
Further Information

Publication History

Received: 13 June 2014

Accepted after revision: 22 September 2014

Publication Date:
29 October 2014 (online)


Abstract

A detailed account regarding the synthesis of 2- and 5-halogenated dopamine is given. The key step is a chemoselective reduction of a nitrostyrene by Zn/HCl at 0 °C. These conditions represent a simple, low-cost alternative to reduction by water-sensitive hydride donors and two-step procedures. Under these conditions, aryl fluoride, chloride, and bromide groups are stable. However, ­iodine undergoes significant reductive dehalogenation.

Supporting Information