- Chemo-, regio-, and stereoselective iron-catalysed hydroboration of alkenes and alkynes
-
The highly chemo-, regio-, and stereoselective synthesis of alkyl- and vinyl boronic esters with good functional group tolerance has been developed using in situ activation of a bench-stable iron(ii) pre-catalyst and pinacolborane (16 examples, 45-95% yield, TOF up to 30000 mol h-1). The first iron-catalysed alkene hydrogermylation is also reported.
- Greenhalgh, Mark D.,Thomas, Stephen P.
-
p. 11230 - 11232
(2013/11/19)
-
- Synthesis and biological evaluation of the mitochondrial complex 1 inhibitor 2-[4-(4-fluorobutyl)benzylsulfanyl]-3-methylchromene-4-one as a potential cardiac positron emission tomography tracer
-
A series of fluorinated chromone analogs with IC50 values ranging from 9 to 133 nM for the mitochondrial complex I (MC-I) has been prepared. A structure-activity relationship (SAR) study of the most potent fluorinated chromone analog 10 demonstrated the linkage heteroatom preference of the side chain region of the molecule while maintaining potent MC-I inhibitory activity. Tissue distribution studies 30 min after [18F]10 administration to Sprague-Dawley (SD) rats demonstrated high uptake of the radiotracer from the blood pool into the myocardium (2.24% ID/g), kidney (1.93% ID/g), and liver (2.00% ID/g). After 2 h about 66% of the activity in the myocardium at 30 min had been retained, whereas ~70% had been cleared from the liver and kidney. MicroPET images of SD rats after [18F]10 administration allowed easy assessment of the myocardium through 60 min with minimal lung or liver interference.
- Radeke, Heike,Hanson, Kelley,Yalamanchili, Padmaja,Hayes, Megan,Zhang, Zhi-Qin,Azure, Michael,Yu, Ming,Guaraldi, Mary,Kagan, Mikhail,Robinson, Simon,Casebier, David
-
p. 4304 - 4315
(2008/03/12)
-
- Contrast agents for myocardial perfusion imaging
-
The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.
- -
-
Page/Page column 43
(2008/06/13)
-