专利号:US-2012178710-A1 优先权日:2009-07-01 标题 :Synthesis of cyclic diguanosine monophosphate and thiophosphate analogs thereof 发明人:JONES ROGER A; GAFFNEY BARBARA L 权利人:JONES ROGER A; GAFFNEY BARBARA L; UNIV RUTGERS 摘要:The invention provides methods for the synthesis of cyclic dinucleotides and thiophosphate analogs thereof as well as a new family of analogs of cyclic diguanosine monophosphate that includes a series of seven phosphorothioate derivatives that includes diastereomers of mono-, di-, and trithiophosphates.
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.
专利号:WO-2024061842-A1 优先权日:2022-09-19 标 题:Improved oligonucleotide synthesis 发明人:CREUSEN GUIDO; MINUTH MARCO; SAMSON DANIEL 权利人:BACHEM HOLDING AG 摘要:A method for the solid-phase synthesis of a target oligonucleotide OT is disclosed, wherein said method comprises a step of incubating a nucleoside or oligonucleotide, which is covalently linked to a solid support and comprises a backbone hydroxyl moiety protected by a di(p-methoxyphenyl)phenylmethyl (DMT) protecting group, with a deprotection mixture, thereby cleaving said protecting group from said nucleoside or oligonucleotide, wherein said deprotection mixture is a liquid composition comprising a solvent, a protic acid having a pKa equal to or smaller than 4, and at least one alcohol of Formula (D), wherein in RD-1 R,D-2 R,D-3 RD-4 and RD-5 are indepently of each other selected from the group consisting of H, OH, a e1-e6-alkyl group, O(C1-C6-aIkyl), C(O)(Ci-C6-alkyl), C(O)O(Ci-C6-alkyl), F, Cl, Br, I, and CN. Such a method does not only suppress depurination, but also results in an acceptable product yield.
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-2025115629-A1 优先权日:2021-03-18 标 题 :Chiral synthons for the synthesis of chiral phosphorothioates 发明人:ZHANG YONGDA; WU LINGLIN 权利人:BOEHRINGER INGELHEIM INT 摘要:This invention relates to compounds of Formula (I) useful as synthons for a general synthetic method for making chiral phosphorothioates, to their preparation and to their use in a robust large scale process for making P-chiral phosphorothioates.