专利号:WO-9323413-A1 优先权日:1992-05-13 标 题:Synthesis of nucleotide monomers 发明人:BEIGELMAN LEONID; MATULIC-ACADEMIC JASENKA 权利人:RIBOZYME PHARM INC 摘要:Methods for synthesis of 2',3'-dideoxycytidine, 2',3'-dideoxyguanosine, 2',3'-dideoxyadenosine, 2',3'-dideoxyinosine and 2',3'-dideoxyguanosine, and 3'-O-benzoyl-2'-deoxyribonucleoside.
专利号:US-6872535-B2 优先权日:1998-05-20 标题:Three-dimensional array of supports for solid-phase parallel synthesis and method of use 发明人:BAUM STEPHEN A 权利人:AVENTIS PHARMA INC 摘要:A three-dimensional (3D) array of solid-phase supports is adapted to provide parallel synthesis of a library of molecules with 3D diversity. Individual locations in the 3D array may be assigned to selected molecules in the library such that molecules may be synthesized at and retrieved from such locations. Also, the supports include aperture walls in stacked plates; the supports may be suspended within stacked plate apertures; the 3D array include discrete supports arranged in columns in one or more wells; the supports include tube inner walls or be suspended in tubes, the tubes being secured in stacked, two-dimensional (2D) frameworks; or the supports include beads contained in porous enclosures having non-porous side walls and being secured in stacked, 2D frameworks. A support transfer device enables transfer of solid-phase supports used in a 3D array. Such apparatus includes: a rack of rods sized to be inserted through supports and a mechanism to prevent supports from coming off the rack; tubes connected to a vacuum manifold to suction supports one Z plane at a time; or a transfer block having recesses to receive one or more support and at least one gate withholding supports from passing through the gate when in a closed position. A method of 3D synthesis includes: a) functionalizing solid-phase supports; b) placing supports in a 3D array; and c) performing parallel synthesis with 3D diversity. At least one unique R 1 group member may be assigned to each Z plane.
专利号:WO-2024185775-A1 优先权日:2023-03-06 标 题:Long-chain alkenyloxy–substituted benzoyl derivative and oligonucleotide synthesis method using same 发明人:OKADA YOHEI; INANAGA KAZATO; SHOJI Yukiya; MIZUFUNE HIDEYA; SUDO TATSUYA; ADACHI Sota; HOSOI Kazushi 权利人:SPERA PHARMA INC; TOKYO UNIV OF AGRICULTURE AND TECHNOLOGY 摘要:The purpose of the present invention is to provide a novel pseudo–solid phase protecting group that can be used in liquid-phase oligonucleotide synthesis. The purpose of the present invention is also to provide an oligonucleotide synthesis method that uses a novel pseudo–solid phase protecting group. The present invention provides a compound represented by formula (1) (in which R represents a C14–60 alkenyl group, n represents 2 or 3, m represents 0 or 1, p represents 1 or 2, X represents C, N, O, or S, Y represents a single bond or B(CH 2 ) t * or may form a ring with X, and Z represents a single bond or (CH 2 ) s (s being an integer from 1 to 5)). The present invention also provides an oligonucleotide production method that uses the compound.
专利号:WO-2022220019-A1 优先权日:2021-04-16 标题 :Long-chain dna synthesis using non-natural base 发明人:MASAKI YOSHIAKI 权利人:TOKYO INST TECH 摘要:The purpose of the present invention is to provide a method for synthesizing a long-chain nucleic acid (particularly DNA) with high accuracy. The present invention provides a method for synthesizing a long-chain nucleic acid, the method comprising using: (i) a nucleoside-3'-O-phosphoramidite derivative having a non-natural nucleic acid base; or (ii) a nucleoside-3'-O-phosphoramidite derivative having a non-natural nucleic acid base and a nucleoside-3'-O-phosphoramidite derivative having a natural nucleic acid base in the chemical synthesis of a nucleic acid based on the phosphoramidite method.
专利号:WO-2025082632-A1 优先权日:2023-10-16 标 题:Method and composition for oligonucleotide synthesis 发明人:SAITO MASAHARU 权利人:BACHEM HOLDING AG 摘要:The invention pertains to a method for the synthesis of oligonucleotides using pseudo solid-phase protecting groups, wherein said method comprises a step of subjecting a solution comprising a component (C-0)# to one or more aqueous extractions, wherein the organic phase comprises the component (C-0)#. Said component (C-0)# is a nucleoside or an oligonucleotide, which is covalently bonded to a pseudo solid-phase protecting group and comprises a free backbone hydroxyl group. The aqueous phase of each of said one or more aqueous extractions has a pH-value in the range of 4-7.
专利号:EP-4605403-A1 优先权日:2022-10-17 标 题:Method and composition for oligonucleotide synthesis 发明人:SAITO MASAHARU; TAKEDA KAZUTAKA; OKADA YOHEI; LUTHER ANATOL 权利人:BACHEM HOLDING AG 摘要:The invention pertains to methods for the synthesis of oligonucleotides using pseudo solid-phase protecting groups, wherein said method comprises at least one aqueous extraction carried out in the presence of one or more amide solvents SA, wherein each amide solvent SA is an amide solvent comprising one or more alkyl groups, wherein these one or more alkyl groups together comprise in total 6−24 carbon atoms. The invention further pertains to compositions comprising an oligonucleotide which is covalently bonded to a pseudo solid-phase protecting group and a mixed solvent comprising on or more of the aforementioned amide solvents SA.
[参考文献]: Son T Nguyen, Et Al. Structure-Activity Relationships Of A Novel Pyranopyridine Series Of Gram-Negative Bacterial Efflux Pump Inhibitors. Bioorg Med Chem. 2015 May 1;23(9):2024-34.
合成参考文献
摘要:Kleoff, M.; Omoregbee, K.; Zimmer, R., Science of Synthesis Knowledge Updates, (2018) 4, 211.