Stereocontrolled synthesis of LNA dinucleoside phosphorothioate by the oxathiaphospholane approach

The application of the oxathiaphospholane approach for the stereocontrolled synthesis of LNA dinucleoside phosphor-othioate is described. The reaction of ring opening condensation proceeds in CH3CN solution in high yield and with over 96% stereoselectivity. One of diastereomers of LNA dinucleoside phosphorothioate (presumably Rp) was found to be readily digested by svPDE. (C) 2001 Elsevier Science Ltd. All rights reserved.