专利号:WO-2008101515-A1 优先权日:2007-02-22 标 题:New synthons for the synthesis of chiral peptide nucleic acids and methods for preparing the same 发明人:BIONDI FABIO 权利人:NANODREAM S R L UNIPERSONALE; BIONDI FABIO 摘要:Novel l-acyl-3-amino-4-hydroxymethylpyiÏ„olidine derivatives useful as PNA synthons optionally having protecting groups suitable of removal under mild conditions are disclosed having the formula (E) wherein: R1 is H or R-C(=O), wherein R is straight or branched alkyl, aryl, substituted aryl including from 1 to 5 heteroatoms, a heterocyclic group including from 1 to 3 heteroatoms; R2 is H, a linker bonded to a solid support, or R6-0-C(=0), wherein R6 is an alkyl or substituted alkyl group having a tertiary carbon atom bonded to the oxygen, CHn-Arm-n wherein n is 1 or 2 and m is 2 or 3 and Ar is aryl or substituted aryl, and R3 is a nucleobase selected from thymine I, cytosine II, adenine III, guanine IV, uracil V, xanthine VI and hypoxanthine VII, a derivative of said nucleobases I-VII protected at the reactive functionalities NH2 or imidic NH, a deazacarbocyclic derivative of said nucleobases I-VII optionally protected at the reactive functionality NH2. Also disclosed are novel intermediates useful for the preparation of the aforementioned PNA synthons, as well as to methods for preparing the intermediates and the final synthons. The latter can be useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers.
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-5256811-A 优先权日:1991-05-23 标 题:Certain intermediates for the preparation of neuinic acid derivatives 发明人:TODD RICHARD S; REEVE MAXWELL 权利人:BRITISH BIO TECHNOLOGY 摘要:compounds of formula I ##STR1## wherein R 1 represents a C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 3-8 cycloalkyl(C 1-8 )alkyl, C 1-8 hydroxyalkyl, C 1-8 alkylthio, phenyl or substituted phenyl; n R 3 represents a C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, CO2(C 1-8 )alkyl, CO 2 (C 2-8 ) alkenyl, C 1-8 alkylthio, (C 1-2 )alkyl CO 2 (C 1-8 ) alkyl or C 1-8 aldehydroalkyl where the aldehyde function is protected by a suitable protecting group (for example, an acetal such as a dimethyl acetal); n R 4 represents a hydrogen atom, C 1-8 alkyl or C 2-8 alkenyl; n Z represents a group (CH 2 ) n or a branched alkyl chain; n n is 1 to 8; n and each of a, b and c is independently a single or a double bond; n can be prepared relatively easily and in good xxx at room temperature by reacting a compound of general formula II ##STR2## wherein R 2 , R 3 , R 4 , Z, a, b and c are as define din general formula I; with a compound of general formula III n n CHI.sub.2 R.sup.1 (III) n n wherein R 1 is as defined in general formula I; n in the presence of metal ions such as chromium (II) ions. The sever conditions of the Wittig reaction can therefore be avoided. n Compounds of formula I are useful intermediates in the synthesis of mevinic acids, which are potent inhibitors of HMG-CoA reductase and which are useful in the treatment of hypocholesterolaemia an hyperlipidaemia.
参考标题:Non-Peptidic Inhibitors Of Human Neutrophil Elastase: The Design And Synthesis Of Sulfonanilide-Containing Inhibitors 作者:Katsuhiro Imaki,Takanori Okada,Yoshisuke Nakayama,Yuuki Nagao,Kaoru Kobayashi,Yasuhiro Sakai,Tetsuya Mohri,Takaaki Amino,Hisao Nakai,Masanori Kawamura |发布日期:1996.12 摘要:A Novel Series Of Pivaloyloxy Benzene Derivatives Has Been Identified As Potent And Selective Human Neutrophil Elastase (Hne) Inhibitors. Convergent Syntheses Were Developed In Order To Identify The Inhibitors Which Are Intravenously Effective In An Animal Model. A Compound Of Particular Interest Is The Sulfonanilide-Containing Analogues. Structure-Activity Relationships Are Discussed. Structural Requirements