专利号:WO-2024182268-A1 优先权日:2023-02-27 标 题 :Liquid phase peptide support synthesis of peptides and peptidomimetics 发明人:HAN AMY 权利人:REGENERON PHARMA 摘要:The present invention provides compounds useful as support for liquid phase organic synthesis e.g., liquid phase organic synthesis of peptides and peptidomimetics. In one aspect, the present invention provides a compound having a structure of Formula (I) where R1, R2, R3, m, and n are as described herein and methods of making and using same.
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-2025282813-A1 优先权日:2021-04-09 标 题 :Pseudo solid phase protecting group and methods for the synthesis of oligonucleotides and oligonucleotide conjugates 发明人:OKADA YOHEI; SUZUKI HIDEAKI; LUTHER ANATOL 权利人:BACHEM HOLDING AG 摘要:A novel pseudo solid phase protecting group and methods for the synthesis of oligonucleotides and oligonucleotide conjugates are provided. The pseudo solid phase protecting group is represented by formula II wherein: * indicates the point of attachment to an oxygen atom of a hydroxyl moiety of the nucleoside, the nucleotide, the oligonucleotide, or of the conjugate of a nucleoside, a nucleotide or an oligonucleotide to be protected; c is 0 or 1; a is an integer of 1 to 12; R3 is H; R5 is O—R6 or H, where R6 is a C8-C40 aliphatic hydrocarbon group; each of R4 is independently O—R6, where R6 is at each occurrence independently a C8-C40 aliphatic hydrocarbon group; b is 1 to 3; with the proviso that if b is 1, at least one of R3 and R5 is not H; and with the further proviso that the sum of all carbon atoms contained in the R3, R4, and R5 moieties present is larger than 23 and smaller than 200.
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.
专利号:WO-2024083746-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.
专利号:US-9284348-B2 优先权日:2005-09-20 标 题:Method for synthesis of peptide using a carrier 发明人:CHIBA KAZUHIRO; KIM SHOKAKU; KONO YUSUKE 权利人:JITSUBO CO LTD 摘要:Disclosed are a carrier for use for separation purpose and a method for separation of a compound which enable a chemical reaction to be performed in a liquid phase, enable a compound of interest to be separated from the liquid phase after the completion of the reaction readily, enable the separated compound to be evaluated by structural analysis or the like while the compound being bound to the carrier, and enable the compound to be separated from the carrier readily. A carrier for separation which has a reaction site capable of reacting with other compound on a benzene ring, and a long-chain group having a specified carbon atom(s) at each of the ortho-position and the para-position of the reaction site through an oxygen atom.
参考标题:Development Of An Efficient Liquid-Phase Peptide Synthesis Protocol Using A Novel Fluorene-Derived Anchor Support Compound With Fmoc Chemistry; Ajiphase® 作者:Daisuke Takahashi,Takashi Yamamoto |发布日期:2012.4 摘要:The Development Of A Novel Fluorene-Type Anchor Support Molecule And A Liquid-Phase Peptide Synthesis Protocol (Ajiphase®) Is Reported. With This Support Molecule, The Synthesis Of A Protected Peptide With A Free Carboxyl Group Could Be Carried Out By Repeated Coupling/deprotection Reactions And Isolation By Simple Precipitation. Cleavage Is Performed Under Mild Acidic Conditions (2% Tfa/chcl3 Or
合成参考文献
摘要:Wu, F.; Zhu, S., Science of Synthesis Knowledge Updates, (2020) 1, 178. 参考文献:10.1007/s10661-021-09302-9 摘要:Srinivasan A, Maruthavanan T, Mayildurai R, Ramasubbu A. GC–MS investigations of VOCs in South Indian honey samples as environmental biomarkers. Environmental Monitoring and Assessment. 2021 Jul 30;193(8):539. doi: 10.1007/s10661-021-09302-9.