124716-09-2

Upstream product

• 78635-98-0 3'-O-levulinoylthymidine 
• 224186-67-8 5'-O-(4,4'-dimethoxytrityl)-3'-O-levulinyl dithymidyl 2-cyanoethyl phosphate 
• 98796-51-1 5'-O-(4,4'-dimethoxytrityl)-2'-deoxythymidine-3'-O-[O-(2-cyanoethyl)-N,N'-diisopropylphosphoramidite] 
• 40615-39-2 5'-O-(4-4'-dimethoxytrityl)thymidine 
• 187539-25-9 C₄₉H₅₄N₅O₁₅PS 

Relevant academic research and scientific papers

ALKOXYPHENYL DERIVATIVE, NUCLEOSIDE PROTECTOR AND NUCLEOTIDE PROTECTOR, OLIGONUCLEOTIDE MANUFACTURING METHOD, AND SUBSTITUENT GROUP REMOVAL METHOD

PROBLEM TO BE SOLVED: To provide an alkoxyphenyl derivative capable of synthesizing oligonucleotide by a liquid phase synthesis method easier and quicker than conventional ones, a nucleoside protector and a nucleotide protector to which the alkoxyphenyl derivative binds, a manufacturing method of oligonucleotide using the same, and a selective removal method of the alkoxyphenyl derivative part, or the like. SOLUTION: There is provided a compound represented by the general formula (1), or a derivative thereof. In the formula, R is each independently substituted/unsubstituted C10 to 40 alkyl; m is an integer of 1 to 5; a plurality of RO may be different when m is 2 or more; X is O, S, NH or NRN; n is an integer of 1 to 4; RN is substituted/unsubstituted C1 to 6 alkyl. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPOandINPIT

Alkoxyphenyl derivative, a nucleotide protected nucleoside protection and, oligonucleotide production, and, removal of substituents (by machine translation)

[A] can be synthesized by a liquid phase synthetic method for oligonucleotide which more easily and quickly made and Tag nucleosides nucleotides, oligonucleotides using the methods of manufacture, the alkoxyphenyl derivative of the selective elimination method, and, like those used for Tag agent. The partial structure represented by the formula [a] have Tag, Tag-nucleoside or nucleotide. (In the formula, R is, independently, a straight chain or branched, alkyl group of carbon number 10 - 40. The m, an integer of 1 - 5. M is 2 or more in the case, a plurality of same RO, or, may be different. The X, O, S, NH, or, NRN Representing. The n, an integer of 1 - 4. RN The, may be substituted, an alkyl group of carbon number 1 - 6 represent. The *, or a mono or oligonucleotides represents a mono or [origonukureoshido[origonukureoshido] binding site. )[Drawing] no (by machine translation)

Investigation of a facile synthetic method for phosphorothioate dimer synthons in oligonucleotide phosphorothioates synthesis

A facile synthetic method of a phosphorothioate dimer block was investigated. Dinucleoside phosphite triester intermediates were obtained in one-pot synthesis by the coupling of a protected nucleoside bearing free 5'- OH and a protected nucleoside bearing free 3'-OH in the presence of phosphorous trichloride (PCl3) and 1,2,4-triazole. The intermediates were easily sulfurized to afford the desired phosphorothioate dimer blocks in 33- 64% overall yields.

Synthesis of dimer phosphoramidite synthons for oligodeoxyribonucleotide phosphorothioates using diethyldithiocarbonate disulfide as an efficient sulfurizing reagent

An efficient solution phase synthesis of deoxyribonucleoside phosphorothioate dimers utilizing phosphoramidite approach is described. Diethyldithiocarbonate disulfide (DDD) was found to be an efficient sulfurizing reagent in the conversion of phosphite triesters to phosphorothioate triesters.

Improved impurity profile of phosphorothioate oligonucleotides through the use of dimeric phosphoramidite synthons

Phosphorothioate oligonucleotides synthesized through assembly of dimeric phosphoramidite synthons show a significantly improved impurity profile compared to oligomers synthesized through coupling of standard monomer phosphoramidites. A greater than 70% reduction of the (n-1)-mer population and a ca. 50% reduction of phosphodiester linkages has been achieved.