Patent ID: 6403781
Filing Date: 2002-06-11
Classification: C07H

Abstract:
A method for synthesizing a phosphorothioate oligonucleotides on a solid phase support comprising the steps of:reacting a phosphordiamidite of formula: wherein:R1 is a protecting group; R2 and R3 are dialkylamino or morpholino; B is a nucleosidic base; R6 is halogen, O-alkyl, O-alkylamino, O-alkylalkoxy, protected O-alkylamino, O-alkylaminoalkyl, O-alkyl imidazole, or a polyether of the formula (O-alkyl)m, where m is 1 to about 10; with a support-bound synthon of formula: wherein:R4 is a linker connected to a solid support; R5 is a phosphoryl protecting group; n is 0 to 100; to form a support-bound phosphoramidite of formula: protecting the support-bound phosphoramidite, thereby forming a support-bound phosphite of formula: sulfurizing the support-bound phosphite to form a protected phosphorothioate; anddeprotecting the protected phosphorothioate to form a further support-bound synthon wherein n is increased by 1.