Compound having structure derived from mononucleoside or mononucleotide, nucleic acid, labeling substance, and method and kit for detection of nucleic acid
A single nucleotide and compound technology, applied in biological testing, biochemical equipment and methods, sugar derivatives, etc., can solve problems such as increased fluorescence intensity
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[0261] The method for producing the compound and nucleic acid of the present invention is not particularly limited, and known synthesis methods (production methods) can be suitably used. For example, in the case of the compound represented by the formula (21), it can be produced by a production method comprising the following steps: after activating the carboxyl group of the compound represented by the following formula (26), it is combined with tris(2-aminoethyl group) amine reaction; protection of amino group; and the reaction of protecting the hydroxyl group present in the compound obtained above with a protecting group, and the reaction of adding a phosphoric acid or phosphoramidite group to the hydroxyl group present in the obtained compound.
[0262] [Chemical 52]
[0263]
[0264] In formula (26), A represents a hydrogen atom or a hydroxyl group. B represents a residue of adenine, guanine, cytosine, thymine or uracil.
[0265] The production method (synthesis metho...
Embodiment 1-3
[0320] According to the following scheme 1, compounds 102 and 103 in which two active amino groups were each protected with a trifluoroacetyl group were synthesized (produced), and phosphoramidite 104 was further synthesized.
[0321] [Chemical 53]
[0322]
[0323] plan 1
[0324] Reagents and reaction conditions (a) (i) N-hydroxysuccinimide, EDC / DMF, (ii) tris(2-aminoethyl)-amine / CH 3 CN, (iii) CF 3 COO Et, Et 3 N; (b) DMTrCl / pyridine; (c) 2-cyanoethyl-N,N,N',N'-tetraisopropylphosphoramidite, 1H-tetrazole / CH 3 CN.
[0325] Regarding Scheme 1 above, it is described in more detail below.
Embodiment 1
[0326] Example 1: 2-[2-[N,N-bis(2-trifluoroacetylaminoethyl)]-aminoethyl]carbamoyl-(E)-vinyl]-2'-deoxyuridine
[0327] Synthesis of (2-[2-[N,N-bis(2-trifluoroacetamidoethyl)]-aminoethyl]carbamoyl-(E)-vinyl)-2′-deoxyuridine, compound 102)
[0328]Starting material (E)-5-(2-carboxyvinyl)-2'-deoxyuridine ((E)-5-(2-carboxyvinyl)-2'-deoxyuridine, compound 101) according to Tetrahedron1987, 43, 20 , 4601-4607 Synthesis. That is, first, 71 mL of 1,4-dioxane was added to 430 mg of palladium(II) acetate (FW224.51) and 1.05 g of triphenylphosphine (FW262.29), and then 7.1 mL of triethylamine (FW 101.19, d=0.726), heated and stirred at 70°C. When the reaction solution changed from reddish brown to dark brown, add 14.2g 2'-deoxy-5-iodouridine (FW354.10) and 7.0mL methyl acrylate (FW 86.09, d=0.956) in 1,4-diox The suspension in alkanes was heated to reflux at 125°C for 1 hour. Afterwards, it was filtered while still hot, the residue was washed with methanol, and the filtrate was recov...
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