ISSN 1017-2548(Print)
ISSN 2234-8530(Online)
Volume 49, Number 4
JKCSEZ 49(4)
August 20, 2005 

^99mTc-Labeled N-(3-bromo-2,4,6-trimethylacetanilido)-iminodiacetic acid (^99mTc-mebrofenin) has been used to assess the functional integrity of the hepatobiliary system. A fast and convenient procedure was established for the synthesis of mebrofenin and radiochemical labeling with ^99mTc. 3-Bromo-2,4,6-trimethylacetanilide was synthesized in large scale under microwave irradiation (300 W, 5 min) by acylation (60% yield) and bromination (96% yield). And it was treated with the disodium salt of iminodiacetic acid under microwave irradiation (300 W, 20 min) to afford mebrofenin in 86% yield. The attractive feature in this procedure involves microwave irradiation that results in shorter reaction times, higher yields, cleaner reaction products and an easier work-up than classical heating. The synthesis time of 2,4,6- trimethylacetanilide was reduced from 1 h to 5 min; the synthesis time of 3-bromo-2,4,6-trimethylacetanilide was reduced from 24 h to 5 min; the synthesis time of mebrofenin was reduced from 48 h to 20 min, when compared with that of the conventional method. Iminodiacetic acid of mebrofenin is a metal complexing moiety that strongly binds ^99mTc. ^99mTc-Mebrofenin between the reduced technetium, prepared by a stannous reduction of the pertechnetate ion, and mebrofenin was formed under microwave irradiation (300 W, 1 min). The synthesis time of ^99mTc-mebrofenin was reduced from 30 min to 1 min, when compared with that of the conventional method. 99.5% of Labeling ef ficiency (LE) of ^99mTc-mebrofenin was determined by using radio-TLC.