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-7060818-B2 优先权日:2003-02-21 标题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process 发明人:HORWITZ COLIN P; GHOSH ANINDYA 权利人:UNIV CARNEGIE MELLON 摘要:An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate. Following deprotection, the diamide diamine intermediate is reacted with an activated diacid, such as an activated malonate, oxalate or succinate derivative to form the macrocyclic tetraamido compound. The macrocyclic tetraamido compound may further be complexed with a transition metal.
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.
专利号:US-2004167329-A1 优先权日:2003-02-21 标 题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process
专利号:WO-2004076425-A1 优先权日:2003-02-21 标题:Improved synthesis of macrocyclic tetraamido compounds and new metal insertion process
专利号:WO-9710263-A1 优先权日:1995-09-12 标 题 :Actinomycin d analogues 发明人:TONG GLENN; NIELSEN JOHN 权利人:AUDA PHARMACEUTICALS APS; TONG GLENN; NIELSEN JOHN 摘要:The present invention relates to new compounds being structurally and functionally similar to Actinomycin D and to combinatorial libraries of such compounds. The Actinomycin D analogues according to the present invention comprise two linear or cyclic peptide moieties constituted by α-amino acids, β-amino acids and/or longer chain φ-amino acids, and a difunctional group which preferably is a cyclic entity, in particular, an aromatic or heteroaromatic entity acting as an intercalator group. Specific compounds and a library of such compounds may be prepared using conventional solid phase peptide synthesis (SPPS) methodologies. The novel compounds are expected to have affinity for DNA and RNA, and libraries thereof may therefore advantageously be used for screening purposes. Furthermore, a novel double-combinatorial technique that may be used in the preparation of librairies of broader classes of compounds has been developed.
[参考文献]: M. Yoon, Et Al. 2,3-Diphenylmaleic Anhydride, An Analogue Of Cis-Stilbene. Acta Cryst. (1995). C51, 1374-1377 [参考文献]: M Pawlowska, Et Al. Sensitive Enantiomeric Separation Of Aliphatic And Aromatic Amines Using Aromatic Anhydrides As Nonchiral Derivatizing Agents. J Chromatogr A. 1994 Apr 22;666(1-2):485-91.
合成参考文献
参考文献:10.1038/ja.2011.55 摘要:Chen X, Zhu X, Ding Y, Shen Y. Antifungal activity of tautomycin and related compounds against Sclerotinia sclerotiorum. J Antibiot (Tokyo). 2011 Aug;64(8):563–9. doi: 10.1038/ja.2011.55.