197004-98-1Relevant academic research and scientific papers
Phenolic analogues of amino carboxylic acid ligands for 99mTc. V* N-benzyl-2-(2-hydroxyphenyl)glycines (bhpg) N-benzyl-2-(4-hydroxyphenyl)glycines (isobhpg)
Gerald Wilson,Katsifis, Andrew G.
, p. 583 - 587 (2000)
A series of tridentate ligands, N-benzyl-2-(2-hydroxyphenyl)glycines (bhpg) (4), were prepared by the Mannich reaction of phenol and a number of para-substituted phenols with glyoxylic acid and benzylamine. When the two ortho positions of the phenol were blocked, as in the case of 2,6-dimethyl and 2,6-dichloro phenols, the isomeric compounds N-benzyl-2-(4-hydroxyphenyl)glycines (isobhpg) (5) were formed. When the phenol had one ortho substituent, as in the case of o-cresol and o-chlorophenol, both isomers were isolated. Two examples of the use of the chiral α-phenylethylamine in place of benzylamine are described. CSIRO 2000.
Synthesis, attempted kinetic resolution and evaluation of [123I]-MK-447 analogues as inflammation radiopharmaceuticals
Siu, Anna F. M.,Lambrecht, Richard M.,Shani, Jashovam,Pyne, Stephen G.,Kane-Maguire, Leon A. P.
, p. 711 - 729 (2007/10/03)
The non-steroidal anti-inflammatory agent 2-amino-methyl-4-tert-butyl-6-iodophenol hydrochloride (MK-447) and some of its analogues were labelled with 123I and tested in an inflamed rat-paw model. Even though MK-447 has a significant anti-inflammatory activity, and a 2.3 ratio for inflamed site over muscle, its usefullness for scintigraphic detection of inflammation is hindered by its high uptake in the skin. The kinetic resolution of diastereomeric products with chiral dienyl iron complexes was unsuccessful as the signals from the respective 1H and 13C NMR spectra were coincident.
