Process for the preparation of oligonucleotides

Details Process for the preparation of oligonucleotides Process for the preparation of oligonucleotides

C - Chemistry, Metallurgy

07

H

260/229.1, 195/1

C07H 21/00 (2006.01) C07F 9/26 (2006.01) C07H 19/04 (2006.01)

Patent

CA 1234060

Abstract of the disclosure The invention relates to a process for the prepa- ration of oligonucleotides by the following steps: reaction of a nucleoside with a phosphine derivative, reaction of the nucleotide derivative thus obtained with a nucleoside bonded to a polymeric carrier, oxidation of the carrier-bound nucleoside-nucleotide thus obtained with formation of phosphotriester groups, blocking of free primary 5'-OH groups, elimination of a protec- tive group from the terminal 5'-OH group, where approp- riate single or multiple repetition of the abovemen- tioned steps to introduce further nucleoside phosphate or oligonucleoside phosphate units, and cleavage of the nucleoside-carrier bond and, where appropriate, elimina- tion of all protective groups present in the oligonucleo- side phosphates. The phosphine derivative used is a compound of the general formula III Image (III) in which X and L can react with OH groups of the sugar units in the oligonucleotides, and R3 is a protective group which can be liberated by .beta.-elimination.

461270

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