Diastereocontrolled synthesis of phosphorothioate DNA via an oxazaphospholidine approach using a novel class of activators, dialkyl(cyanomethyl)ammonium salts.

摘要

Dialkyl(cyanomethyl)ammonium salts 1 were synthesized and used as a novel class of activators for the stereospecific condensations of diastereopure nucleoside 3'-O-oxazaphospholidines with a nucleoside. This new oxazaphospholidine method could efficiently produce both (Rp)- and (Sp)-dinucleoside phosphorothioates.