General Papers ARKIVOC 2015 (v) 34-43
Page 34
©
ARKAT-USA, Inc
Palladium-catalyzed coupling reactions for the preparation of
concatenated azoles
Delia Hernández,*
a
C. Giovana Granados,
b
Esmeralda Sánchez,
a
Fernando Albericio,
c,d
and Mercedes Álvarez*
,c,e
a
Química Orgánica y Biotecnología, Facultad de Ciencias Químicas, Universidad Veracruzana,
Orizaba, Veracruz, México
b
Unidad de Diseño y Síntesis de Biomoléculas, Departamento de Química, Centro de
Investigación y de Estudios Avanzados (CINVESTAV-IPN), México, D.F.
c
Institute for Research in Biomedicine, Barcelona Science Park-University of Barcelona, Baldiri
Reixac 10, 08028 Barcelona, Spain
d
Department of Organic Chemistry, University of Barcelona, 08028 Barcelona, Spain
e
Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona, 08028
Barcelona, Spain
E-mail: mercedes.alvarez@irbbarcelona.org
DOI: http://dx.doi.org/10.3998/ark.5550190.p009.017
Abstract
The coupling reactions mediated by sp
2
-sp
2
transition metals, mostly Pd, allowed the
chemoselective preparation of some synthetic compounds and intermediate structures of great
complexity. This work describes the methodology used to obtain several derivatives with
bisoxazole and thiazole-oxazole units. The required organozinc reagents were prepared from n-
BuLi and ZnCl
2
, and the bimetallic derivative of ethyl oxazole-4-carboxylate was obtained by a
second transmetalation with CuI.
Keywords: Organometallic, oxazole, thiazole, transmetalation, coupling reactions
Introduction
In recent decades, some marine natural products have been found to be an important source of
new bioactive compounds and drug leads. The chemical structures of marine products with
heterocycles, such as 2,4´-bisoxazole, trisoxazole and 2,4´-thiazole-oxazole, substituted in
different positions of the ring are common in different families of natural products (Figure 1).