Tetrahedron letters

5-(Benzylmercapto)-1H-tetrazole as activator for 2′-O-TBDMS phosphoramidite building blocks in RNA synthesis

R Welz, S Müller

文献索引：Welz, Ruediger; Mueller, Sabine Tetrahedron Letters, 2002 , vol. 43, # 5 p. 795 - 797

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被引用次数: 81

摘要

An improved method for the preparation of 5-(benzylmercapto)-1H-tetrazol as activator in RNA synthesis is described. Reaction of benzylthiocyanate with azide delivers the corresponding tetrazole with 72% yield under optimised conditions. We demonstrate that 5- (benzylmercapto)-1H-tetrazol is a superior activator of 2′-O-TBDMS phosphoramidite building blocks. Compared to routinely used 1H-tetrazol, application of a 0.25 M 5-( ...