专利号:WO-9740025-A1 优先权日:1996-04-19 标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA 摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-5817751-A 优先权日:1994-06-23 标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives 发明人:SZARDENINGS ANNA KATRIN; CAMPBELL DAVID 权利人:AFFYMAX TECH NV 摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.
专利号:US-2003159164-A1 优先权日:1998-05-29 标 题:Compositions and methods for the synthesis of fatty acids, their derivatives and downstream products 发明人:KOPCHICK JOHN JOSEPH; KELDER BRUCE; HUANG YUNG-SHENG; KIRCHNER STEPHEN J; MUKERJI PRADIP 摘要:The invention generally relates to synthesis of essential fatty acids and their derivatives, long-chain polyunsaturated fatty acids (LC-PUFAs) and eicosanoids in transfected cells and in transgenic animals.
专利号:US-6803468-B2 优先权日:2000-08-29 标 题 :Process for the synthesis of n-(5-methylnicontinoyl)-4 hydroxypiperidine, a key intermediate of rupatadine 发明人:KUMAR YATENDRA; PRASAD MOHAN; SINGH SHAILENDRA KUMAR 权利人:RANBAXY LAB LTD 摘要:The present invention relates to an improved and industrially advantageous process for the preparation of N-(5-methylnicotinoyl)-4-hydroxypiperidine of Formula I, as shown in the accompanied drawings. This compound is a key intermediate for the synthesis of rupatadine, a potent dual antagonist of histamine and platelet-activating factor (PAF).
专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-6756199-B1 优先权日:1994-02-23 标题:Peptide nucleic acid combinatorial libraries and improved methods of synthesis 发明人:COOK PHILLIP DAN; KIELY JOHN; SPRANKLE KELLY 权利人:ISIS PHARMACEUTICALS INC 摘要:New sub-monomer synthetic methods for the preparation of peptide nucleic acid oligomeric structures are disclosed that provide for the synthesis of both predefined sequence peptide nucleic acid oligomers as well as random sequence peptide nucleic acid oligomers. Further these methods also provide for the incorporation of peptide nucleic acid units or strings of such units with amino acids or strings of amino acids in chimeric peptide nucleic acid-amino acid compounds. Further disclosed are method of making random libraries of peptide nucleic acids using the fully preformed monomers. Chimeric oligomers and libraries of the same are also disclosed.
参考标题:On The Synthesis Of Platelet-Activating Factor Via Acetylation Of 1-Alkyl-Sn-Glycero-3-Phosphocholine. Formation Of Structural Isomer Of Paf In The Presence Of Bases 作者:V.V Chupin,O.V Ostapenko,V.N Klykov,M.V Anikin,G.A Serebrennikova |发布日期:1996.6 摘要:Shown That Platelet-Activating Factor (Paf) Specimens Prepared Via Acetylation Of 1-Alkyl-Sn-Glycero-3-Phosphocholine (Lyso-Pf) With Acetic Anhydride Are Heterogeneous. The Contaminated Compound Was Isolated And Identified To Be The Structural Isomer Of Paf, 1-Alkyl-3-Acetyl-Sn-Glycero-2-Phosphocholine (Iso-Paf). It Appeared, That Iso-Paf Is Formed When Performing The Reaction In The Presence Of Organic
合成参考文献
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