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CAS号16653-19-3 N-(苄氧基)邻苯二甲酰亚胺 | CAS号2687-43-6 苄氧基胺盐酸盐 | CAS号100-51-6 苯甲醇 | CAS号100-44-7 氯化苄 | CAS号100-39-0 溴化苄 | CAS号67-62-9 O-甲基羟胺 | CAS号100-63-0 苯肼 | CAS号497-25-6 2-恶唑烷酮 | CAS号3532-25-0 N-phenylmethoxy... | CAS号115364-82-4 [1-[(benzyloxy)... | CAS号100-46-9 苄胺 | CAS号2048-52-4 4-amino-1-pheny... | CAS号22426-89-7 4-methoxy-N-phe... | CAS号106-40-1 对溴苯胺 | CAS号140-11-4 乙酸苄酯 | CAS号103-50-4 二苄醚 | CAS号100-51-6 苯甲醇N-苯基甲氧基氨基甲酸乙酯置于氢氧化钾体系中,用 甲醇 作为反应溶剂,化学反应生成 O-苄基羟胺
参考文献:O,N-取代羟基胺.2. Mitteilung.o-(苯基烷基)-羟胺的合成与本征交换(untersuchungenübersynthetische Arzneimitteln Ii)
标题:O,N-取代羟基胺.2. Mitteilung.o-(苯基烷基)-羟胺的合成与本征交换(untersuchungenübersynthetische Arzneimitteln Ii)
摘要:Es Wirdüber合成,化学与物理化学化学反应,合成o-(苯基烷基)-羟胺胺.盐酸氢硼酸甘油酯,位于羟基苯并二苯并二恶英,C-Atome得到了保护,氢已被氨化,氨氮磷铵.letztere Wurden Zum Teil气相色谱法和鉴定方法.分子式:A-(1-甲基-2-苯基-乙基)-羟基lamin-盐酸盐:氯化铵,丙苯酮(72%)和甲基苄基酮(28%).o-(2-苯基-乙基)-羟基lamin-盐酸盐:氯化铵和2,5-二苯基-1,4-二恶烷;o-(1-甲基-2-苯基-乙基)-N-甲基-羟基lamin-盐酸盐:甲胺盐酸盐,丙炔酮(59.4%)和甲基-苄基酮(40.6%);
DOI:10.1002/hlca.19620450502
专利信息
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:EP-0671928-B1
优先权日:1992-09-24
标题 :Synthesis of n-substituted oligomers
发明人:ZUCKERMANN RONALD N; KERR JANICE M; KENT STEPHEN BRIAN HENRY; MOOS WALTER H; SIMON REYNA J; GOFF DANE A
权利人:CHIRON CORP
摘要:Poly N-substituted Glycines (poly NSGs), wherein the substituents bear purine or pyrimidine bases (R<9>) every second glycine: In addition, a solid phase method for the synthesis of N-substituted oligomers of more general structures is disclosed.The poly NSGs obtainable by this method 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 the 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-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.
专利号:US-6063919-A
优先权日:1998-08-14
标题:Process for the synthesis of exochelins
发明人:GAUDIOSO LARRY A; WEGLARZ MICHAEL A
权利人:KEYSTONE BIOMEDICAL INC
摘要:A process for the synthesis of an Exochelin comprising the steps of generating L-N-[(2-benzyloxy-(benzoyl)] serine or L-N-[2-benzyloxy (benzoyl)] threonine, creating L-N-t-Boc- epsilon -hydroxynorleucine and reacting same to produce L-N-Boc- epsilon -bromonorleucine trimethylsilylethyl ester, providing a dicarboxylic acid and forming an O-benzyl methyl hydroxamate from the dicarboxylic acid, coupling the O-benzyl methyl hydroxamate with the L-N-Boc- epsilon -bromonorleucine trimethylsilylethyl ester to give an L-N2-Boc-N6-methyl,N6-(benzyloxy) lysine 2-trimethylsilylethyl ester which incorporates the dicarboxylic acid as modified above, removing the N-tert-butoxycarbonyl protecting group from the L-N2-Boc-N6-methyl, N6-(benzyloxy) lysine 2-trimethylsilylethyl ester to yield a substituted lysine, and coupling the same with the L-N-[2-benzyloxy (benzoyl) serine or -threonine to yield a 2-trimethyl silylethyl ester of dibenzyl Exochelic acid, transforming the 2-trimethyl silylethyl ester of dibenzyl Exochelic acid to dibenzyl Exochelic acid, preparing benzyl epi-cobactin, forming an ester bond between the dibenzyl Exochelic acid and benzyl epi-cobactin to form an intermediate, and, hydrogenolytically removing three benzyl groups from said intermediate, resulting in the synthesized Exochelin. More particularly, a synthesis for Exochelin 786SM (R) is disclosed wherein the dicarboxylic acid is suberic acid and the serine form is utilized.
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-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.