Strap yourself in with this week’s front cover highlighting the work of Ishwar Singh and co-workers who have developed a fast, strain promoted cycloaddition as a tool for RNA conjugation on the solid phase exploiting the cycloaddition of a series of RNA-cyclooctynes with both azide (strain-promoted azide–alkyne cycloaddition) and nitrile oxide dipoles (strain-promoted nitrile oxide–alkyne cycloaddition). Singh et al. say that the reaction is compatible with 2’-OMe blocking as well as with 2’-O-TBDMS protection on the ribose moieties of the sugar.
Fast RNA conjugations on solid phase by strain-promoted cycloadditions
Ishwar Singh, Colin Freeman, Annemieke Madder, Joseph S. Vyle and Frances Heaney
Ming-Jung Wu and colleagues, National Sun Yat-sen University, have developed an efficient synthetic method to convert enynylpyrazoles to pyrazolo[1,5-a]pyridines and 6-iodopyrazolo[1,5-a]pyridines by gold-catalyzed cyclisation and iodinemediated cyclisation reactions, respectively. Wu et al. go on to demonstrate the synthetic utility of this by preparing a p38 kinase inhibitor.
Au(I)-catalyzed and iodine-mediated cyclization of enynylpyrazoles to provide pyrazolo[1,5-a]pyridines
Hung-Chou Wu, Chia-Wen Yang, Long-Chih Hwang and Ming-Jung Wu
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