CAS: 6232-88-8; 4-Bromomethylbenzoic Acid

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CAS号99-94-5 对甲基苯甲酸 | CAS号589-18-4 4-甲基苄醇 | CAS号104-87-0 对甲基苯甲醛 | CAS号17201-43-3 α-溴对甲基苯甲腈 | CAS号589-29-7 对苯二甲醇 | CAS号876-07-3 4-溴甲基苯甲酰溴 | CAS号94-08-6 对甲基苯甲酸乙酯 | CAS号26496-94-6 4-(溴甲基)苯甲酸乙酯 | CAS号106-38-7 对溴甲苯 | CAS号52780-16-2 4-溴甲基苯甲酰氯 | CAS号55715-03-2 4-溴甲基-3-硝基苯甲酸 | CAS号50685-26-2 4-(氰甲基)苯甲酸 | CAS号141884-92-6 4-bromomethyl-3... | CAS号146781-28-4 4-乙氧基甲基苯甲酸 | CAS号501-89-3 4-羧基苯乙酸 | CAS号51359-78-5 4-溴甲基苯甲醛 | CAS号223507-96-8 SOTS-1 (technic... | CAS号24239-07-4 2-[4-(bromometh... | CAS号3006-96-0 4-羟甲基苯甲酸 | CAS号28149-48-6 4-(二乙氧基次膦基甲基)苯甲酸

对苯二甲醇置于镍,过氧化苯甲酰 N-溴代丁二酰亚胺(Nbs),氢气体系中,用 四氯化碳,Sodium Hydroxide 作为反应溶剂,化学反应 0.5H,反应生成 对溴甲基苯甲酸
参考文献:Selective Hydrogenolysis Of Bis(Hydroxymethyl)Aromatic Compounds
标题:Selective Hydrogenolysis Of Bis(Hydroxymethyl)Aromatic Compounds
摘要:在碱性溶液中,采用raney镍对对称双(羟甲基)芳香化合物进行选择性氢解,温度为20°C,时间为24至36小时.对应单氢解产物的产率在75%至96%之间.通过合成4-(溴甲基)苯甲酸,展示了该反应的实用性.
DOI:10.1055/s-1992-26346

专利信息

专利号:US-6683189-B1
优先权日:1996-02-26
标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
发明人：DERVAN PETER B; BAIRD ELDON
权利人:CALIFORNIA INST OF TECHN
摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.

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:WO-9817677-A1
优先权日:1996-10-24
标 题 :Improvements in solid-phase synthesis of peptides and related compounds
发明人：ENGLEBRETSEN DARREN
权利人:UNIV QUEENSLAND; ENGLEBRETSEN DARREN
摘要:The invention relates to spacers for use in solid-phase synthesis of peptides and peptide-related compounds, in which a spacer construct is used to ensure that the target peptide or peptide-related compound is at a distance equivalent to at least 5-15 amino acids from the solid support. Constructs of the invention are particularly applicable to the synthesis of strongly hydrophobic peptide, which are otherwise difficult, if not impossible to purify and analyse. The constructs and methods of the invention are also applicable to synthesis of peptide nucleic acids.

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-4101721-A
优先权日:1976-12-09
标题 :Solid phase synthesis of protected peptides
发明人：RICH DANIEL H; GURWARA SWEET K
权利人:WISCONSIN ALUMNI RES FOUND
摘要:The invention is addressed to the preparation of 3-nitro-4-bromomethyl benzoic acid, as a new compound from which 3-nitro-4-bromomethyl benzoyl amide polystyrene resin can be prepared for solid synthesis of protected peptide acids and amides and separation thereof without cleavage of acid labile protecting groups or decomposition of aromatic acid groups and from which purified polypeptides can be formed.