CAS: 106-57-0; Piperazine-2,5-Dione

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106-57-0 5625-52-5 4526-77-6

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聚甘氨酸 以 乙二醇 用作溶剂,化学反应 3.0H,以75%的收率获得甘氨酸酐
参考文献:通过不对称氢化反应选择性合成手性取代的 2,4-二酮咪唑烷和 2,5-二酮哌嗪
标题:通过不对称氢化反应选择性合成手性取代的 2,4-二酮咪唑烷和 2,5-二酮哌嗪
摘要:已经开发了在温和条件下由 Rh/ F-Spirophos 络合物催化的 5-亚烷基-2,4-二酮咪唑烷(乙内酰脲)和 3-亚烷基-2,5-酮哌嗪的对映选择性氢化,这提供了一种高效的方法.手性乙内酰脲和 2,5-酮哌嗪衍生物的对映选择性合成,对映选择性高达 99.9% Ee.
Doi:10.1021/acs.Orglett.1C01894

专利信息

专利号:WO-2009107771-A1
优先权日:2008-02-27
标题:Method for synthesis of peptide using gold-iron oxide composite nanoparticle
发明人：KOGA YUICHI; YAMAMOTO TAKAO A; SEINO SATOSHI; TAKANO KAZUFUMI; TOHNAI NORIMITSU; KUWABARA MASAYUKI
权利人:UNIV OSAKA; KOGA YUICHI; YAMAMOTO TAKAO A; SEINO SATOSHI; TAKANO KAZUFUMI; TOHNAI NORIMITSU; KUWABARA MASAYUKI
摘要:Disclosed is a method for the synthesis of a peptide by using a gold-iron oxide composite nanoparticle. Particularly disclosed are: a composite nanoparticle-peptide complex which can be screened with a magnetic force; and an advantageous method for the synthesis of a peptide library composed of the composite nanoparticle-peptide complex. The method for the synthesis of a peptide comprises the steps of: adsorbing a linker molecule on the surface of gold in a gold-iron oxide composite nanoparticle; and synthesizing the peptide through the linker molecule by employing solid-phase peptide synthesis. The method for the synthesis of a peptide library comprises the steps of: adsorbing a linker molecule on the surface of gold in a gold-iron oxide composite nanoparticle; and synthesizing the peptide through the linker molecule by employing split synthesis.

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-5977301-A
优先权日:1992-09-24
标题 :Synthesis of N-substituted oligomers
发明人：ZUCKERMAN RONALD N; KERR JANICE M; KENT STEPHEN B H; MOOS WALTER H; SIMON REYNA J; GOFF DANE A
权利人:CHIRON CORP
摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.

专利号:US-5789577-A
优先权日:1994-12-30
标 题 :Method for the controlled synthesis of polynucleotide mixtures which encode desired mixtures of peptides
发明人：GEYSEN H MARIO
权利人:CHIRON CORP
摘要:A method to obtain selected individual polynucleotides or mixtures thereof each of which encodes a peptide and at least one polynucleotide of the mixture encodes a peptide having a target property. The polynucleotides of the invention present in the mixture in detectable, retrievable, and clonable amounts are expressed in a host organism for screening for the target activity. The invention features the ability to synthesize controlled random polynucleotides to produce a predetermined mixture of polynucleotides and to avoid synthesis of a stop codon by adjusting the proportions into which the synthesis pool is subdivided and by adjusting the proportions of activated nucleotides added at each coupling step. A polynucleotide encoding a peptide having a target property can be selected and sequenced to deduce the amino acid sequence of the peptide.

专利号:US-7723082-B2
优先权日:2002-06-21
标题 :Polynucleotides and polypeptides coded by said polynucleotides involved in the synthesis of diketopiperazine derivatives
发明人：GONDRY MURIEL; GENET ROGER; LAUTRU SYLVIE; PERNODET JEAN-LUC
权利人:COMMISSARIAT ENERGIE ATOMIQUE; CENTRE NAT RECH SCIENT
摘要:The invention concerns novel isolated natural or synthetic polynucleotides and polypeptides coded by said polynucleotides, involved in the synthesis of diketopiperazine derivatives, vectors comprising said polynucleotides, micro-organisms transformed with said polynucleotides, uses of said polynucleotides and said polypeptides, as well as methods for the synthesis of diketopiperazine derivatives, including cyclodipeptides and diketopiperazine derivatives 3- and 6-substituted by α,β-unsaturated amino acid side chains.

专利号:US-5877278-A
优先权日:1992-09-24
标题:Synthesis of N-substituted oligomers
发明人：ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA
权利人:CHIRON CORP
摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.