Title : Lipase mediated synthesis of modified bicyclic nucleosides
Abstract:
Over two decades, a large number of nucleosides have been synthesized, which demonstrated potent antiviral and antitumour activities and have become cornerstones of treatment for patients with cancer or viral infections. Oligonucleotide-based antisense strategies represent a unique paradigm for the treatment of a wide variety of human diseases. In order to discover new class of nucleoside derivatives with enhanced biological activities, the modifications in the sugar moietiy have been attempted, which provide a remarkable level of control over nucleoside sugar puckering and its biological activity.
Herein, we report; the selective biocatalytic acetylation studies on modified 3′-azido-4′-C-hydroxymethylated sugar derivatives with an aim to develop an efficient and easy method for the synthesis of ribo-azido/amino LNA monomers and xylo-azido/amino spiro-oxetano nucleosides and the selective biocatalytic deacetylation studies on modified 3′-azido-4′-C-acetoxymethylated sugar derivatives with an aim to develop an efficient and easy method for the synthesis of ribo-azido/amino spiro-oxetano nucleosides and xylo-azido/amino LNA monomers.
