Domino ReactionsAn efficient, metal-free, multipathway coupled domino strategy for the construction of 2-acyloxazoles from various substrates, which include methyl ketones, arylethenes, and arylacetylenes, is described by An-Xin Wu and co-workers in their Full Paper on page 638 ff. This process is a logical approach by a consecutive iodination/Kornblum oxidation/cyclization sequence. This transformation is an example of the self-organization and logical synthesis of organic compounds and derivatives in domino, cascade, and tandem reactions.
C-H ActivationNitrogen-based ligands are uniquely reactive in palladium-catalyzed direct arylations of heteroarenes. In their Focus Review on page 624 ff., Fumitoshi Shibahara and Toshiaki Murai discuss the diverse applications of this combination and how such systems have solved problems, such as low reactivity at certain positions on heterocyclic rings, that are difficult to address by the use of other commonly used ligands, such as phosphines.
b-Lactam AntibioticsPenicillins belong to the family of b-lactam antibiotics, which kill bacteria by inhibiting cell-wall biosynthesis. It is commonly thought that a free carboxyl group is required in the drug structure for effective recognition by and inhibition of the target penicillin-binding proteins (PBPs). Penicillin esters are usually inactive, but the 2-nitrobenzyl penicillinates described by Jacqueline Marchand-Brynaert and co-workers in their Full Paper on page 654 ff. unexpectedly depart from the rule and are good inhibitors. The magic effect of the 2-NO 2 group could be attributable to strong stabilizing interactions in the PBP active site.
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