CAS: 79-08-3; Bromoacetic Acid

上下游产品

CAS号64-19-7 冰醋酸 | CAS号598-21-0 溴乙酰溴 | CAS号407-25-0 三氟乙酸酐(TFAH) | CAS号82191-81-9 β-brom°Caproic acid | CAS号75-05-8 乙腈 | CAS号558-13-4 四溴化碳 | CAS号141-78-6 乙酸乙酯 | CAS号96-32-2 溴乙酸甲酯 | CAS号105-36-2 溴乙酸乙酯 | CAS号79-11-8 氯乙酸 | CAS号105401-90-9 2-(4-methyl-2-p... | CAS号105190-52-1 2-bromo-1-(2,3,... | CAS号10574-68-2 3-propan-2-yl-2... | CAS号33445-07-7 异丙氧基乙酸 | CAS号3785-34-0 1,2-双(溴乙酰氧基)乙烷 | CAS号37478-58-3 2-(哌嗪-1-基)乙酸 | CAS号59564-59-9 3,4-二氢喹喔啉-2(1H)-酮 | CAS号103-50-4 二苄醚 | CAS号5437-45-6 溴乙酸苄酯 | CAS号3480-87-3 3-羟基-3-苯基丙酸

溶剂黄146置于copper(I) Bromide体系中,用 乙酸乙酯 作为反应溶剂,化学反应生成 溴乙酸
参考文献:新型的芳基取代的嘧啶酮类化合物在结肠癌中具有3-巯基丙酮酸硫转移酶的抑制作用.
标题:新型的芳基取代的嘧啶酮类化合物在结肠癌中具有3-巯基丙酮酸硫转移酶的抑制作用.
摘要:3-巯基丙酮酸硫转移酶(3-Mst)是最近发现的哺乳动物h 2 S来源之一.最近的一项研究发现了几种具有微摩尔效价的新型3-Mst抑制剂.其中,(2-[((4-羟基-6-甲基嘧啶-2-基)硫烷基]-1-(萘-1-基)乙-1-酮)或hmpsne是最有效和选择性最大的.现在,我们以该化合物的核心为原料,分别对嘧啶酮和芳基酮进行了修饰.合成了63种化合物的文库;测试化合物的h 2从重组3-Mst体外产生s.随后测试活性化合物以阐明其效能和选择性.计算机建模研究已经描述了绑定到3-Mst的活动站点所必需的一些关键结构特征.在基于细胞的试验中测试了六种新型3-Mst抑制剂:它们对鼠mc38和ct26结肠癌细胞的增殖具有抑制作用;还证实了具有最高效力和最佳基于细胞的活性的化合物的抗增殖作用(1B)对小鼠mc38肿瘤的生长.
DOI:10.1021/acs.Jmedchem.1C00260

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-8822702-B2
优先权日:2002-12-20
标 题 :Synthesis of amines and intermediates for the synthesis thereof
发明人：BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL
权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE
摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.

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-2008287649-A1
优先权日:2006-12-29
标 题 :Methods for the synthesis of cyclic peptides
发明人：CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R
权利人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R
摘要:Methods for the synthesis of cyclic peptides are provided, as well as novel dipeptide compounds. The methods include the solid phase synthesis of a dipeptide, which is the coupled to a second peptide in a solid phase reaction. The peptide is then cyclized following the coupling reaction. The methods and dipeptides are particularly useful for the synthesis of MC-4 receptor agonist peptides.

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-7462714-B2
优先权日:2002-09-24
标题 :Process for the industrial synthesis of the methyl diester of 5-amino-3-carboxymethyl-4-cyano-2-thiophenecarboxylic acid, and application to the synthesis of bivalent salts of ranelic acid and their hydrates
发明人：VAYSSE-LUDOT LUCILE; LECOUVE JEAN-PIERRE; LANGLOIS PASCAL
权利人:SERVIER LAB
摘要:Process for the industrial synthesis of the compound of formula (I): n nApplication to the synthesis of bivalent salts of ranelic acid and more especially strontium ranelate and its hydrates.