Recently, transition-metal-catalyzed C-H functionalization has attracted tremendous interest as a valuable tool for carbon-carbon and carbon-heteroatom bond formation. However, due to the inertness of C(sp 3)-H bonds and the difficulty to achieving high selectivity among the many chemically similar entities in a given molecule, the selective activation of C(sp 3)-H bonds remains a great challenge. The recent progress in transition-metal-catalyzed arylation of unactivated C(sp 3)-H bonds assisted by bidentate directing groups is reviewed, including the scope of reactions, mechanism and synthetic applications.
A series of novel 2-substituted-1,5-benzothiazepines were synthesized successfully and their structures were determined by elemental analysis, IR, MS/HRMS and 1 H NMR. The synthetic conditions of 2-substituted-4-aryl-1,5-benzothiazepines were investigated. The antifungal activities of these 2-substituted-1,5-benzothiazepine derivatives were tested and the results confirmed that the 2-ethyl carboxylate was necessary for antifungal activity in 1,5-benzothiazepine compounds 1.
A simple, mild, and high yielding procedure for the iodination of alcohols using a combination of NaBH 4 and I 2 is described. The effectiveness of the protocol is achieved with benzylic alcohols and primary alkylic alcohols whereas allylic and secondary alcohols are found to be unreactive.
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