PROCESS FOR PRODUCING OLIGONUCLEOTIDES

摘要

PCT No. PCT/EP84/00244 Sec. 371 Date Jun. 18, 1985 Sec. 102(e) Date Jun. 18, 1985 PCT Filed Aug. 10, 1984 PCT Pub. No. WO85/00816 PCT Pub. Date Feb. 28, 1985.The invention relates to a process for the preparation 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 protective group from the terminal 5'-OH group, where appropriate single or multiple repetition of the abovementioned steps to introduce further nucleoside phosphate or oligonucleoside phosphate units, and cleavage of the nucleoside-carrier bond and, where appropriate, elimination of all protective groups present in the oligonucleoside phosphates. The phosphine derivative used is a compound of the general formula III (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.