Takeda Pharmaceutical Company Limited

Takeda Pharmaceutical Company Limitjed

Mitsuru Nonogawa

Tsuneo Yasuma

Toshiaki Nagata

Hideki Saito

In this method, an oligonucleotide represented by formula (II) [wherein Y, Q, Base, r and r' are each as defined in claim] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R, Y, Base, Z, Ar, R, Rand n are each as defined in claim]. 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&#x2032;-direction but also in the 5&#x2032;-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide. 

Method for liquid-phase synthesis of nucleic acid

In this method, an oligonucleotide is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R, Y, Base, Z, Ar, R, Rand n are each as defined in Claim]. 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 cars dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3'-direction but also in the 5&#x2032;-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide. 

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Osaka, Japan

Mitsuru Nonogawa