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:US-6632950-B2 优先权日:2000-07-06 标 题:Process for the preparation of derivatives of 4-amino-3-hydroxypyrrole-2-carboxylic acid 发明人:PHILLION DENNIS P; SINGH MEGH 权利人:PHARMACIA CORP 摘要:Novel processes and intermediates are provided for the synthesis of derivatives of 4-amino-3-hydroxypyrrole-2-carboxylic acids that are useful as monomers for polyamides capable of binding dsDNA. According to one preferred reaction scheme, an alkyl alkoxymethylene nitroacetate (Formula VIII) is prepared by reaction of a trialkyl orthoformate or orthoacetate with a nitroacetate ester in the presence of a carboxylic anhydride. The compound of Formula VIII is condensed with an N-substituted glycine to yield an N-substituted (2-nitro-2-alkoxycarbonyl)vinyl glycinate ester (Formula VII). Ring closure in the presence of an alkali metal alkoxide yields a 4-nitro-3-hydroxypyrrole-2-carboxylic ester (Formula V). After blocking of the 3-hydroxy group to produce a further intermediate (Formula IV), the 4-nitro group is reduced to a 4-amino group (Formula III), and the 4-amino group is then blocked by reaction with a dicarbonate diester to produce the fully blocked intermediate (Formula II). Saponification of the 2-carboxylic acid ester yields a monomer having a free 2-carboxylic ester moiety (Formula I).
专利号:US-2024425461-A1 优先权日:2023-06-13 标题 :Preparation process of intermediate, synthesis process of amino imidazole carboxylate ester and hplc purity measure method 发明人:DUAN JIANXIN; LU ZHAOQIANG; FAN JINWEI; HUANG QUNHUI; ZHANG YANJUN; CHEN WEISU; QIN WEI 权利人:ASCENTAWITS PHARMACEUTICALS LTD 摘要:This invention relates to a process for preparing an intermediate of aminoimidazole carboxylate, a process for synthesizing aminoimidazole carboxylate and an HPLC method for determining purity. The process of preparing the intermediate of aminoimidazole carboxylate comprises subjecting a compound of formula I-2 and a formate as the reactants to a first-step reaction in a benzene solvent and at a temperature of −5° C.−5° C., with the addition of a solution of sodium alkoxide in such a way that the temperature of the reaction solution is not higher than 5° C., to obtain the intermediate of aminoimidazole carboxylate or a mixture comprising a compound of formula I-3, i.e., the intermediate of aminoimidazole carboxylate. By using a sodium alkoxide reagent, as a comparatively safe alternative to NaH and potassium tert-butoxide which are prone to cause fire hazards or explosions and are not suitable for use in large-scale production, the process of the present application can ensure smooth progression of the reaction to the product and effectively improve the overall safety of the reaction without noticeably impairing the reaction efficiency.
专利号:WO-9724361-A1 优先权日:1995-12-29 标 题 :Nucleotide analogs 发明人:ARIMILLI MURTY N; BISCHOFBERGER NORBERT W; JONES ROBERT J; LEE WILLIAM A; PRISBE ERNEST J 权利人:GILEAD SCIENCES INC; ARIMILLI MURTY N; BISCHOFBERGER NORBERT W; JONES ROBERT J; LEE WILLIAM A; PRISBE ERNEST J 摘要:Nucleotide phosphonate esters characterized by the presence of an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise an ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
专利号:US-7439350-B2 优先权日:1993-09-17 标题 :Nucleotide analogs 发明人:BISCHOFBERGER NORBERT W; JONES ROBERT J; ARIMILLI MURTY N; LIN KUEI-YING; LOUIE MICHAEL S; MCGEE LAWRENCE R; PRISBE ERNEST J; LEE WILLIAM A; CUNDY KENNETH C 权利人:GILEAD SCIENCES INC 摘要:Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
专利号:US-5886179-A 优先权日:1993-09-17 标 题 :Nucleotide analogs 发明人:ARIMILLI MURTY N; BISCHOFBERGER NORBERT W; JONES ROBERT J; LEE WILLIAM A; PRISBE ERNEST J 权利人:GILEAD SCIENCES INC 摘要:Nucleotide phosphonate esters characterized by the presence of an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise an ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.