Abstract:
Iodoamide derivatives are one of the most privileged structure motifs frequently found in
natural products, pharmaceuticals, functional materials, and medicines. Synthesis and
biological evaluation of Iodoamide derivatives have been a topic of special interest to
organic and medicinal chemist. Here a convenient method for the synthesis of 4,4-
disubstituted and 2,4- disubstituted amide derivatives through palladium catalyzed crosscoupling
reaction and without palladium catalyzed cross-coupling reaction is reported. In
this purpose, 2,6- diiodo – 4 –substituted ,2-iodo-4-substituted, and 2-iodo -6- substituted
anilines 4, 5, 6 were synthesized by the iodination of their parent 4-sustituted and 2 -
substituted anilines using KI, KIO3 in methanol. The cross-coupling reaction of 2,6-
diiodo – 4 –substituted anilines and 2-iodo-4-substituted anilines 4, 5 with acid chloride
were carried out in the presence of (Ph3P)2PdCl2 in MeCN at room temperature for 24-48
hrs. under nitrogen atmosphere to yield N-(2,6-diiodo-4-substituted phenyl)-p-substituted
benzamide and N-(2-iodo-4-substituted phenyl)-p-substituted benzamide 7, 8. Again the
reaction study on 2,6- diiodo–4–substituted, 2-iodo-4- substituted and 2-iodo-6-
substituted anilines e.g.on 4, 5, 6 with acid chlorides were carried out in benzene at room
temperature for 24-48 hrs under N2 atmosphere to yield N-(2,6-diiodo-4-substituted
phenyl)- p-substituted benzamide, N-(2-iodo-4-substituted phenyl)- p-substituted
benzamide and -(2-iodo-6-substituted phenyl)- p-substituted benzamide 7, 8, 9 & 10.-----------------------------------
