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기록

IMPROVED OLIGONUCLEOTIDE SYNTHESIS

발명심사 중
40조회수
21청구항 · 3 독립항
§ Ⅰ

개요

발명자

Guido CREUSEN; Marco MINUTH; Daniel SAMSON

IPC 분류

C7H 1/C7H 21/2

CPC 분류

C7H1/C7H21/2

A method for the solid-phase synthesis of a target oligonucleotide Ois disclosed, wherein said method comprises a step of incubating a nucleoside or oligonucleotide, which is covalently linked to a solid support and comprises a backbone hydroxyl moiety protected by a di(p-methoxyphenyl)phenylmethyl (DMT) protecting group, with a deprotection mixture, thereby cleaving said protecting group from said nucleoside or oligonucleotide, wherein said deprotection mixture is a liquid composition comprising a solvent, a protic acid having a pKa equal to or smaller than 4, and at least one alcohol of Formula (D), wherein in RR,R,Rand Rare indepently of each other selected from the group consisting of H, OH, a e-e-alkyl group, O(C-C-alkyl), C(O)(Ci-C-alkyl), C(O)O(Ci-C-alkyl), F, Cl, Br, I, and CN. Such a method does not only suppress depurination, but also results in an acceptable product yield.

원문 (중국어)

A method for the solid-phase synthesis of a target oligonucleotide Ois disclosed, wherein said method comprises a step of incubating a nucleoside or oligonucleotide, which is covalently linked to a solid support and comprises a backbone hydroxyl moiety protected by a di(p-methoxyphenyl)phenylmethyl (DMT) protecting group, with a deprotection mixture, thereby cleaving said protecting group from said nucleoside or oligonucleotide, wherein said deprotection mixture is a liquid composition comprising a solvent, a protic acid having a pKa equal to or smaller than 4, and at least one alcohol of Formula (D), wherein in RR,R,Rand Rare indepently of each other selected from the group consisting of H, OH, a e-e-alkyl group, O(C-C-alkyl), C(O)(Ci-C-alkyl), C(O)O(Ci-C-alkyl), F, Cl, Br, I, and CN. Such a method does not only suppress depurination, but also results in an acceptable product yield.