125I –Amoxicillin preparation as a guide tracer for inflammation detection

The objective of this study is to label Amoxicillin with radioactive iodine (125I-AC) via direct electrophilic substitution to act as a promising tracer for inflammation imaging. The highest labeling yield of 80% was achieved after studying all the parameters affecting the labeling reaction using Iodogen (IG) as an oxidizing agent. Molecular Modeling Structure was done using MOE program to predict the suitable 125I position. The product structure was established by a cold iodination reaction using Iodine-127. Biological evaluation of (125I-AC) was carried out using groups of inflamed mice with different exogenous agents such as E.Coli and Turpentine oil. The (125I-AC) shows an in vitro stability of about 97% after 24 h.While doing in vivo studies over 4 h, the tracer stability of 99% was observed.

Upper-rim functionalization and supramolecular polymerization of a feet-to-feet-connected biscavitand

An octaiodobiscavitand was synthesized via an aromatic Finkelstein iodination reaction in good yield. An octa-functionalized biscavitand self-assembled to form a supramolecular polymer in the solid state.

Facile C–H iodination of electron deficient benzodithiophene-S,S-tetraoxide for the development of n-type polymers

A C–H iodination reaction of the electron-poor building block, benzo[1,2-b:4,5-b0]-dithiophene-1,1,5,5-tetraoxide has been reported. This facile functionalization has led to the development of two novel n-type donor–acceptor conjugated polymers.

Synthesis of new pyrrolidine-based organocatalysts and study of their use in the asymmetric Michael addition of aldehydes to nitroolefins

New pyrrolidine-based organocatalysts with a bulky substituent at C2 were synthesized from chiral imines derived from (R)-glyceraldehyde acetonide by diastereoselective allylation followed by a sequential hydrozirconation/iodination reaction. The new compounds were found to be effective organocatalysts for the Michael addition of aldehydes to nitroolefins and enantioselectivities up to 85% ee were achieved.

Palladium-catalyzed picolinamide-directed iodination of remote ortho-C−H bonds of arenes: Synthesis of tetrahydroquinolines

A new palladium-catalyzed picolinamide (PA)-directed ortho-iodination reaction of ε-C(sp2)−H bonds of γ-arylpropylamine substrates is reported. This reaction proceeds selectively with a variety of γ-arylpropylamines bearing strongly electron-donating or withdrawing substituents, complementing our previously reported PA-directed electrophilic aromatic substitution approach to this transformation. As demonstrated herein, a three step sequence of Pd-catalyzed γ-C(sp3)−H arylation, Pd-catalyzed ε-C(sp2)−H iodination, and Cu-catalyzed C−N cyclization enables a streamlined synthesis of tetrahydroquinolines bearing diverse substitution patterns.