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公开(公告)号:EP3786173A1
公开(公告)日:2021-03-03
申请号:EP19792159.6
申请日:2019-04-23
发明人: TANAKA, Yuki , SAITO, Tatsuya , IHARA, Hideki
IPC分类号: C07H19/10 , C07F9/6558 , C07H19/20 , C07H21/02
摘要: The present invention provides an amidite compound represented by formula (1) which enables a synthesis of RNA with high purity, and the method for preparing a polynucleotide by using the same compound. (In the formula (1), wherein R represents the following formula (wherein R a and R b are identical to or different from each other and each represents a methyl group, an ethyl group, or a hydrogen atom, with the proviso that R a and R b does not represent a hydrogen atom. n is an integer of 1 to 5), and B a represents a group containing optionally protected nucleobase structure, and G 1 and G 2 are identical to or different from each other and each represents a protecting group for a hydroxy group, and G 3 are identical to or different from each other and each represents an alkyl group.
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2.
公开(公告)号:EP4049996A1
公开(公告)日:2022-08-31
申请号:EP20879365.3
申请日:2020-08-28
发明人: OSHIRO, Ikuya , SAITO, Tatsuya , IHARA, Hideki
IPC分类号: C07C315/04 , C07C317/22 , C07H19/067 , C12N15/113 , C12N15/115 , C12Q1/68 , C12Q1/6853
摘要: The present invention provides an amidite compound capable of improving a yield and a purity of a polyoligonucleotide, a glycoside compound as an intermediate thereof, and a production method for a polynucleotide using the amidite compound. The present invention also provides an amidite compound of formula (1) capable of improving a yield and a purity of a polyoligonucleotide, a glycoside compound of formula (10) (in formulae (10) and (1), B a , R a , R b , R c , G 1 , G 2 , and G 3 are as defined in the description, and R is represented by the following formulae), and a production method for a polynucleotide using the amidite compound.
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公开(公告)号:EP3848381A1
公开(公告)日:2021-07-14
申请号:EP19856557.4
申请日:2019-09-06
发明人: SAITO, Tatsuya , IHARA, Hideki
IPC分类号: C07H19/067 , C07H19/10 , C07B61/00
摘要: The present invention provides a process for preparing a glycoside compound represented by general formula (3), which comprises the following step: Step A: a step of reacting a glycoside compound represented by general formula (1) with an ether compound represented by formula (2) in the presence of an oxidizing agent and an acid to prepare a glycoside compound represented by general formula (3), wherein the oxidizing agent is added to a reaction system, followed by adding an acid thereto (wherein B a represents a cytosine group which may be optionally substituted with acyl group, or an uracil group, R 1 represents a C1 to C6 alkyl group or a phenyl group, and n is 0 or 1), wherein an oxidizing agent is selected from a group consisting of N-halogenated succinimide and N-halogenated hydantoin, and an acid is selected from a group consisting of perfluoroalkylcarboxylic acid and salts thereof, alkylsulfonic acid and salts thereof, arylsulfonic acid and salts thereof, perfluoroalkylsulfonic acid and salts thereof, and any combinations of two kinds or more thereof, which can provide a synthesis of a desired compound (an amidite compound) with high purity.
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公开(公告)号:EP4043476A1
公开(公告)日:2022-08-17
申请号:EP20874517.4
申请日:2020-08-28
发明人: SAITO, Tatsuya , IHARA, Hideki
IPC分类号: C07H23/00
摘要: A purpose of the present invention is to provide a method for producing a glycoside compound having a high purity. The present invention provides a method for producing a glycoside compound represented by formula (3) (wherein B a , i-Pr and n are the same as those defined below), which comprises reacting a glycoside compound of formula (1) (wherein B a represents an adenine group which may be optionally substituted with an acyl group, and i-Pr represents an isopropyl group) with an ether compound of formula (2) (wherein R 1 represents a C1-C6 alkyl group or a phenyl group, and n is 0 or 1) in one or more solvents selected from tetrahydropyran and 4-methyltetrahydropyran in the presence of one or more halogenated agents selected from halogen, N-halogenated succinimide, and N-halogenated hydantoin.
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