摘要 |
<p>PURPOSE:To obtain a polynucleotide in high yield and short time without causing side reaction by reacting a nucleoside phosphorous acid ester derivative with a nucleoside in the presence of an imidazolinium compound. CONSTITUTION:The objective polynucleoside is produced by condensing a nucleoside phosphorous acid ester derivative of formula I (A is pyrimidine base or purine base: R<1> is hydroxyl-protecting group or mono or polynucleoside phosphorous acid ester residue; R<2> is H or cationic group) with a nucleoside of formula II (B is pyrimidine base or purine base; R<3> is same as R<1>) in the presence of an imidazolinium compound of formula III (R<4> and R<5> are lower alkyl; X and Y are halogen) in a solvent (e.g. acetonitrile) at room temperature and oxidizing the resultant polynucleoside phosphorous acid ester of formula IV. The amounts of the compound of formula I and the compound of formula III are 1-50mol and 1-250mol per 1 mol of the compound of formula II, respectively.</p> |