专利号:WO-2025215126-A1 优先权日:2024-04-12 标题:Synthesis of vidofludimus and its calcium salt 发明人:VITT DANIEL; IGLICAR PETRA; GEGE CHRISTIAN; Mühler Andreas; KOHLHOF HELLA; GRÖPPEL MANFRED 权利人:IMMUNIC AG 摘要:The invention relates to the process of preparation of 2-fluoro-4-(3-methoxyphenyl)aniline (3) as an intermediate. Said intermediate 2-fluoro-4-(3-methoxyphenyl)aniline (3) is obtained in a Suzuki coupling reaction from (3-methoxyphenyl)boronic acid (1) and 4-bromo-2-fluoro-aniline (2). The invention further relates to the synthesis of vidofludimus (5) from said intermediate 2-fluoro-4-(3-methoxy-phenyl)aniline (3) and from 1-cyclopentene-1,2-dicarboxylic anhydride (4). The invention further relates to the synthesis of vidofludimus calcium (6) from said vidofludimus (5) and from a calcium salt, preferably Ca(OH)2.
专利号:US-7351781-B2 优先权日:2001-04-24 标题 :Synthesis of vinyl polymers by controlled radical polymerization 发明人:WHITE DANIELA; O'DWYER JAMES B 权利人:PPG IND OHIO INC 摘要:A controlled free radical polymerization process, which includes the steps of: adding a monofunctional iniferter compound to an oxygen-free solvent; heating the solution to a temperature sufficient to allow the iniferter compound to form two carbon centered radical residues; adding a first monomer composition comprising one or more monomers to the solution containing the radical containing residues; polymerizing the first monomer composition to form a quasi-living polymer; and optionally polymerizing a second monomer composition comprising one or more monomers, which are different than the first monomer composition. The resulting non-random copolymer having the general formula:n nφ-[-A p -B s -] t -φn nwhere A and B are different compositions of ethylenically unsaturated monomers; p is an integer from 1 to 1,000; s is an integer from 0 to 1,000; t is an integer from 1 to 100; and φ is a residue from the iniferter.
专利号:US-8138272-B2 优先权日:2006-05-22 标 题:Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds 发明人:KONRADI ANDREI W; SMITH JENIFER L 权利人:KONRADI ANDREI W; SMITH JENIFER L; ELAN PHARM INC 摘要:This invention provides an improved synthesis of polymer conjugates of formula (I), n nof agricultural, therapeutic, and food additive compounds. In particular, a process is described for the preparation of conjugates by treating primary or secondary alcohol substituents of active compounds with polymeric nucleophiles using “Mitsunobuâ€? or related reaction conditions.
专利号:US-2003018151-A1 优先权日:2001-04-24 标题 :Synthesis of vinyl polymers by controlled radical polymerization
专利号:WO-02085957-A1 优先权日:2001-04-24 标 题:Synthesis of vinyl polymers by controlled radical polymerization
专利号:WO-9729091-A1 优先权日:1996-02-09 标题:Balanol analogues 发明人:NIELSEN JOHN; LYNGSOE LARS OLE 权利人:AUDA PHARMACEUTICALS APS; NIELSEN JOHN; LYNGSOE LARS OLE 摘要:The present invention relates to a solid phase methodology for the preparation of a combinatorial library of structural analogues of the natural product balanol (ophiocordin, azepinostatin), which is a protein kinase C (PKC) and protein kinase A (PKA) inhibitor. The method comprises solid-phase synthesis of the analog variants of balanol whereby a high molecular diversity is introduced. The synthetic scheme is based on a retrosynthetic analysis of the native structure which revealed three main building blocks suitable as templates for modification. The dicarboxy-functional moiety can be immobilised to the polymer support either as the monoallyl ester or as the internal anhydride. The libraries produced by the method are especially suited for high throughput screening of potential drug candidates for the treatment of mammals, especially humans.