专利号:US-10730904-B2 优先权日:2012-11-14 标 题:Method for liquid-phase synthesis of nucleic acid 发明人:NONOGAWA MITSURU; NAGATA TOSHIAKI; SAITO HIDEKI; YASUMA TSUNEO 权利人:TAKEDA PHARMACEUTICALS CO 摘要:In this method, an oligonucleotide represented by formula (II) [wherein Y 1 , Q, Base, r and r′ are each as defined in claim 1 ] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R 1 , Y, Base, Z, Ar, R 2 , R 3 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.
专利号:US-6040439-A 优先权日:1997-09-05 标题 :Method for chemical synthesis of oligonucleotides 发明人:HAYAKAWA YOSHIHIRO; KATAOKA MASANORI 权利人:JAPAN SCIENCE & TECH CORP 摘要:The present invention provides a practical method capable of chemically synthesizing a 100-mer or more long-chain oligonucleotide easily and reliably and a novel compound used in said method. The present invention relates to a method for chemical synthesis of an oligonucleotide by the phosphoroamidite method, which comprises preparing a base moiety-unprotected nucleoside phosphoroamidite from a base moiety-unprotected nucleoside by use of an imidazole trifluoromethanesulfonate represented by the following chemical formula, and coupling said base moiety-unprotected nucleotide phosphoroamidite in a predetermined order to chemically synthesize an oligonucleotide consisting of a specific nucleotide sequence, as well as to an imidazole trifluoromethanesulfonate represented by the chemical formula. ##STR1##
专利号:US-7122693-B2 优先权日:1988-04-11 标题 :Acetaldehyde acetal compounds, their synthesis, and uses thereof 发明人:BELLEAU EXECUTRIX OF ESTATE PI; DIXIT DILIP M; NGUYEN-BA NGHE 权利人:SHIRE BIOCHEM INC 摘要:The acetaldehyde compounds, 2-thiobenzoylacetaldehyde diethylacetal, 2-benzoyloxyacetaldehyde bis(2-methoxyethyl)acetal, 2-hydroxyacetaldehyde bis( 2-methoxyethyl)acetal, 2-thiobenzoylacetaldehyde bis(2-methoxy-ethyl)acetal, and 2-thioacetaldehyde bis(2-methoxyethyl)acetal, are useful as intermediates in the synthesis of substituted 1,3-oxathiolanes and substituted 1,3-dioxolanes.
专利号:US-2023212204-A1 优先权日:2020-01-16 标题:Reagents and their use for modular enantiodivergent synthesis of c-p bonds 发明人:XU DONGMIN; RIVAS-BASCÓN NAZARET; KNOUSE KYLE W; PADIAL NATALIA; ZHENG BIN; VANTOUROUT JULIEN; SCHMIDT MICHAEL; EASTGATE MARTIN D; BARAN PHI 权利人:BRISTOL MYERS SQUIBB CO; SCRIPPS RESEARCH INST 摘要:The disclosure describes chiral P(V)-based reagents and their uses for the modular, scalable, and stereospecific synthesis of chiral phosphines, phosphine oxides and particular oligonucleotides.
专利号:US-2008206850-A1 优先权日:2007-02-28 标 题:Methods and compositions for DNA synthesis 发明人:DELLINGER DOUGLAS J; DELLINGER GERALDINE F; CARUTHERS MARVIN H 权利人:DELLINGER DOUGLAS J; DELLINGER GERALDINE F; CARUTHERS MARVIN H 摘要:In some embodiments, the present disclosure relates to new phosphoramidite compositions, that have Silyl-containing carbonate or thiocarbonate or ether as 5′-hydroxyl protecting groups useful of the synthesis of DNA, and in particular for the synthesis of long sequences of DNA (e.g., >50 mer). In some embodiments, there are provided methods for simultaneous oxidation of the internucleoside phosphate triester linkages and removal of the 5′-hydroxyl-protecting group, making this process a new 2-step DNA synthesis, that involves the use of peroxyanions in combination with fluoride anions.
专利号:US-2008206851-A1 优先权日:2007-02-28 标题:Methods and compositions for RNA synthesis 发明人:DELLINGER DOUGLAS J; DELLINGER GERALDINE F; CARUTHERS MARVIN H 权利人:DELLINGER DOUGLAS J; DELLINGER GERALDINE F; CARUTHERS MARVIN H 摘要:In some embodiments, the present disclosure relates to new phosphoramidite compositions, that have Silyl-containing carbonate or thiocarbonate or ether as 5′-hydroxyl protecting groups useful fo the syntheis of RNA, and in particular for the synthesis of long sequences of RNA (e.g., >50 mer). In some embodiments, there are provided methods for simultaneous oxidation of the internucleoside phosphate triester linkages and removal of the 5′-hydroxyl-protecting group, making this process a new 2-step RNA synthesis, that involves the use of peroxyanions in combination with fluoride anions.
摘要:B.C. Pal. Biochem. 1, 558 (1962). 参考文献:10.1002/cphc.200500692 摘要:Frey JA, Leist R, Müller A, Leutwyler S. Gas-phase Watson-Crick and Hoogsteen isomers of the nucleobase mimic 9-methyladenine x 2-pyridone. Chemphyschem. 2006 Jul 17;7(7):1494–9. doi: 10.1002/cphc.200500692. 参考文献:10.1016/j.jinorgbio.2003.12.003 摘要:Bacac M, Hotze AC, van der Schilden K, Haasnoot JG, Pacor S, Alessio E, Sava G, Reedijk J. The hydrolysis of the anti-cancer ruthenium complex NAMI-A affects its DNA binding and antimetastatic activity: an NMR evaluation. J Inorg Biochem. 2004 Feb;98(2):402–12. doi: 10.1016/j.jinorgbio.2003.12.003. 参考文献:10.1021/ic901508w 摘要:Montagner D, Venzo A, Zangrando E, Longato B. Irreversible insertion of benzonitrile into platinum(II)-nitrogen bonds of nucleobase complexes. Synthesis and structural characterization of stable azametallacycle compounds. Inorg Chem. 2010 Mar 01;49(5):2103–10. doi: 10.1021/ic901508w.