专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-9567315-B1 优先权日:2016-04-22 标 题:Method for synthesis of 4-OH substituted anabaseine derivative 发明人:CHANG YU; HSU CHENG-FANG 权利人:INST NUCLEAR ENERGY RES ATOMIC ENERGY COUNCIL EXECUTIVE YUAN ROC 摘要:A method for synthesis of 4-OH substituted anabaseine derivative which is used as an α 7 receptor agonist is revealed. A nucleophilic substitution reaction of δ-valerolactam with ethyl nicotinate is carried out to get an intermediate product. Then heat the intermediate product under reflux with concentrated hydrochloric acid to get a cyclized product-anabaseine. Next anabaseine and 4-hydroxyethoxy-2-methoxybenzaldehyde are reacted under concentrated hydrochloric acid catalysis to get a 4-OH anabaseine derivative 3-[(4-Hydroxyethoxy-2-methoxy)-benzylidene]anabaseine. The 4-OH anabaseine derivative is synthesized and prepared easily by the present invention. Not only the steps for synthesis are simplified, the yield is as high as 60%. The product can be mass-produced.
专利号:US-7592392-B2 优先权日:2003-04-04 标 题 :Synthesis of functional polymers for use in organic synthesis and combinatorial chemistry 发明人:LINDSLEY CRAIG W; WISNOSKI DAVID D 权利人:MERCK & CO INC 摘要:The present invention relates to a novel process for the preparation of solid-supported scavenging reagents and solid-supported functional polymers. The invention further relates to novel solid-supported functional polymers and to their use in organic synthesis and combinatorial chemistry.
专利号:WO-0168615-A1 优先权日:2000-03-13 标题 :Quinazoline synthesis 发明人:DENER JEFFREY MARK; LEASE TIMOTHY G; NOVACK AARON ROBERT 权利人:CHEMRX ADVANCED TECHNOLOGIES I; DENER JEFFREY MARK; LEASE TIMOTHY G; NOVACK AARON ROBERT 摘要:The present invention relates to a method for making a compound of Formulas I, II and III. The method of the present invention also enables parallel and simultaneous synthesis of a plurality of compounds represented by Formulas I, II and III.
专利号:US-4914151-A 优先权日:1987-05-18 标题:Resin-linker combination for the solid-phase synthesis of peptides and intermediates 发明人:MERGLER MONIKA; GOSTELI JACQUES; GROGG PETER 权利人:BACHEM FEINCHEMIKALIEN AG 摘要:A novel polymeric support resin of the formula I in which R is a lower alkoxy, lower alkythio or group in which R1 and R2 are lower alkoxy, which is crosslinked by means of 0.5 - 2% of an optionally halogen-substituted divinylbenzene is used to prepare peptides and intermediates thereof. Derivatives of this polymeric support resin derived from N alpha - and particularly side chain-protected amino acids of the formula IV are also used to prepare peptides and intermediates thereof.
专利号:US-7056348-B2 优先权日:2001-04-19 标题:5-aryl-1,3,3-trimethyl-2-methylene-indoline derivatives and salts thereof, methods for the production and use of said compounds for the temporary coloration of fibers 发明人:SAUTER GUIDO; BRAUN HANS-JUERGEN; REICHLIN NADIA 权利人:WELLA AG 摘要:A method for the synthesis of 5-aryl-1,3,3,-trimethyl-2-methylene-indoline derivatives of Formula (I) or its salts of Formula (Ia) wherein 1 mole of a 5-aryl-2,3,3-trimethyl-3H-indole derivative of Formula (VII) is reacted for 1 to 44 hours at a temperature of 20° to 180° C. in an apolar, aprotic or polar, protic or polar aprotic solvent with 1 to 50 moles of a compound of Formula R1-A; new compounds of Formulas (I)/(Ia) and (V), obtainable by this method as well as an agent containing at least one compound of Formula (I)/(Ia) and a carbonyl/imine compound for dyeing keratinic fibers and a method for temporarily dyeing keratin fibers, for which the keratin fiber is dyed with the aforementioned agent and the dyeing, so obtained, is removed again at any later time by a sulfite preparation.
参考文献:10.1186/1476-0711-10-23 摘要:Kim JH, Chan KL, Mahoney N, Campbell BC. Antifungal activity of redox-active benzaldehydes that target cellular antioxidation. Annals of Clinical Microbiology and Antimicrobials. 2011 May 31;10(1):23. doi: 10.1186/1476-0711-10-23.