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:WO-2024153752-A1 优先权日:2023-01-20 标 题 :Stereoselective synthesis of intermediates and synthesis of quinagolids 发明人:RYBERG PER; PINESCHI MAURO; COMPARINI LUCREZIA 权利人:FERRING BV 摘要:Disclosed is a method for preparing compounds with improved stereoselectivities. The described compounds are useful intermediates and may find particular application in the synthesis of compounds containing an octahydrobenzoquinoline moiety (e.g. an octahydrobenzo[g]quinoline moiety), such as quinagolide and its derivatives. Also disclosed is a method for stereoselectively (e.g. enantioselectively) preparing an intermediate used in the existing manufacturing process for the synthesis of quinagolide this intermediate also finding utility in the synthesis of other compounds containing an octahydrobenzo[g]quinoline moiety, in particular those having a substituent at the 3- position on the octahydrobenzo[g]quinoline.
专利号:US-10364220-B2 优先权日:2012-12-21 标题:Synthesis of succinimides and quaternary ammonium ions for use in making molecular sieves 发明人:SCHMITT KIRK D; ZUSHMA STEPHEN; BURTON ALLEN W 权利人:EXXONMOBIL CHEMICAL PATENTS INC 摘要:The present invention relates to the synthesis of succinimides, in particular to a method for the synthesis of a succinimide compound, comprising the step of reacting an alkyne, with carbon monoxide and ammonia or an amine, in the presence of an iron catalyst, wherein the reaction is carried out in an amine liquid phase and/or in the absence of an ether solvent. The succinimides may be reduced to quaternary ammonium cations which may be used as structure directing agents in the synthesis of molecular sieves.
专利号:US-7102023-B2 优先权日:1999-11-24 标 题:Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries 发明人:BUCHWALD STEPHEN L; PLANTE OBADIAH J; SEEBERGER PETER H 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.
专利号:US-4108870-A 优先权日:1977-06-06 标 题:Stereocontrolled synthesis of α-multistriatin 发明人:FRIED JOSEF; ELLIOTT WILLIAM J 权利人:UNIV CHICAGO 摘要:A practical stereocontrolled synthesis of a mixture containing a major amount of α-multistriatin and a minor amount of γ-multistriatin in an overall yield of about 73% from cis-2-butene-1,4-diol is provided. α-Multistriatin is one of the three essential components of the aggregation pheromone of the European elm bark beetle.
专利号:US-7767826-B2 优先权日:2007-10-05 标题 :Process for the synthesis of L-(+)-ergothioneine 发明人:TRAMPOTA MIROSLAV 权利人:PHARMATECH INTERNATIONAL INC 摘要:This invention relates to a novel process for the preparation of optically pure L-(+)-ergothioneine. The process for the chemical synthesis of L-ergothioneine comprises steps which consist of reacting L-histidine alkyl ester with an acid halide, chloroformate or pyrocarbonate in the presence of a base, hydrolysis of the alkyl-(S,Z)-2,4,5-triamidopent-4-enoate to obtain a (S)-alkyl 2,5-diamido-4-oxopentanoate, acid catalyzed hydrolysis of the (S)-alkyl 2,5-diamido-4-oxopentanoate followed by reaction with a metal thiocyanate to obtain the thiohistidine, protection of the sulfur of thiohistidine as the tert-butyl thioether, dialkylation of the primary amine to obtain a tertiary amine, quaternization of the tertiary amine, and removal of the protecting group to obtain the desired (S)-3-(2-mercapto-1H-imidazol-5-yl)-2-(trialkylammonio)propanoate (I). This process affords a better yield and is capable of practical application at large scale.