Journal of Labelled Compounds and Radiopharmaceuticals
J Label Compd Radiopharm 2007; 50: 468–470.
Published online in Wiley InterScience
JLCR
Short Research Article
Synthesis of the myoviewTM ligand, [bisphosphinoethane-
1,2-14C]tetrofosminy
GEOFFREY T. WOOLLEY*, SEAN L. KITSON and R. GORDON REID
GE Healthcare Limited, Amersham Place, Little Chalfont, Buckinghamshire HP7 9NA, UK
Received 22 August 2006; Revised 2 November 2006; Accepted 22 November 2006
Abstract: The carbon-14 radiolabels in [bisphosphinoethane-1,2-14C]tetrofosmin ligand were readily introduced by
reacting 1,2-dibromo[U-14C]ethane with bis(2-ethoxyethyl)benzylphosphine (1). This was converted to the
MyoviewTM ligand in an overall yield of 45%. This radiosynthesis was important in obtaining marketing approval
from the regulatory authorities and allowed MyoviewTM to become one of the main heart imaging agents of
today. Copyright # 2007 John Wiley & Sons, Ltd.
Keywords: MyoviewTM; tetrofosmin; gamma emitter; technetium-99m
Introduction
presence or absence of infarction under exercise and
rest conditions (Figure 1).1 This achievement was
recognized by winning the 1998 prestigious Queens
Award for Technical Achievement.2 One reason for the
success of MyoviewTM is that it uses the gamma emitter
technetium-99m rather than thallium-201.3,4
MyoviewTM is used in cardiology as an imaging agent to
study the heart in microscopic detail. The cardiac
imaging agent is labelled with technetium-99m com-
plexed to a biphosphine ligand tetrofosmin or P-53.
MyoviewTM is useful in the diagnosis and localization of
regions of reversible myocardial ischaemia in the
Many different phosphine ligands were prepared and
tested during the development of MyoviewTM and
tetrofosmin was found to be the most superior ligand
(Personal communication, P. G. Edwards, Department
of Chemistry, Cardiff University, UK).5
EtO
OEt
MyoviewTM highlights
P
P
P
EtO
OEt
*
Technetium-99m-labelled drug for myocardial per-
+
99mTc O2
fusion imaging for detection of Coronary Artery
Disease (CAD).6
*
Indicated for use with approved pharmacologic
stress agents for known or suspected CAD.6
EtO
P
OEt
OEt
*
High target-to-background ratio provides clear
images.4,6,7
Improved image clarity provides confident diagnosis.4,8
EtO
*
MyoviewTM
*
Demonstrates good sensitivity, specificity, and diag-
nostic accuracy.8
*
Imaging can begin as soon as 15 minutes or up to
4 hours after administration of MyoviewTM, enhancing
patient management and department flexibility. The
product was approved by the FDA in February 1996.
*Correspondence to: Geoffrey T. Woolley, GE Healthcare Limited, The
Maynard Centre, Forest Farm, Whitchurch, Cardiff CF14 7 YT, UK.
E-mail: geoff.woolley@ge.com
yProceedings of the Ninth International Symposium on the Synthesis
and Applications of Isotopically Labelled Compounds, Edinburgh,
16–20 July 2006.
The MyoviewTM is supplied as a kit containing
*
tetrofosmin, tin chloride and sodium hydrogen
Copyright # 2007 John Wiley & Sons, Ltd.