公开(公告)号：US20150315229A1

公开(公告)日：2015-11-05

申请号：US14442601

申请日：2013-11-13

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Mitsuru NONOGAWA

IPC: C07H19/207 ,  C07H19/16 ,  C07H19/06

CPC classification number: C07H19/207 ,  C07H1/00 ,  C07H19/06 ,  C07H19/067 ,  C07H19/073 ,  C07H19/16 ,  C07H19/167 ,  C07H21/00 ,  C07H21/04

Abstract: In this method, an oligonucleotide is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R1, Y, Base, Z, Ar, R2, R3 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 cars dispense with columm-chromalographic 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.

Abstract translation: 在该方法中，通过使用由式（I）表示的新型核苷单体化合物作为合成单元制备寡核苷酸[其中X，R 1，Y，碱，Z，Ar，R 2，R 3和n各自如上所定义 在权利要求1中]。 该新型核苷单体化合物是一种核苷，其碱基部分被具有至少一个疏水基团的芳烃 - 羰基 - 羰基或硫代羰基取代。 方法汽车在每次反应中均没有色谱 - 色谱纯化，不仅能在3'方向而且在5'方向上实现碱伸长，从而实现寡核苷酸的有效的液相质量合成。

公开(公告)号：US20190135852A1

公开(公告)日：2019-05-09

申请号：US16240677

申请日：2019-01-04

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Mitsuru NONOGAWA ,  Toshiaki NAGATA ,  Hideki SAITO ,  Tsuneo YASUMA

IPC: C07H19/207 ,  C07H19/073 ,  C07H19/167 ,  C07H1/00 ,  C07H19/06 ,  C07H21/04 ,  C07H19/067 ,  C07H19/16 ,  C07H21/00

Abstract: In this method, an oligonucleotide is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R1, Y, Base, Z, Ar, R2, R3 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.