Takeda Pharmaceutical Company Limited
Method for liquid-phase synthesis of nucleic acid

Abstract:

In this method, an oligonucleotide represented by formula (II) [wherein Y.sup.1, Q, Base, r and r' are each as defined in claim 1] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R.sup.1, Y, Base, Z, Ar, R.sup.2, R.sup.3 and n are each as defined in claim 1]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3'-direction but also in the 5'-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide. ##STR00001##