CAS: 1415562-82-1; (R)-(1-(4-((3-Methyl-5-((Phenylsulfonyl)Methyl)Phenoxy)Methyl)Benzyl)Pyrrolidin-2-yl)Methanol

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3,5-Dimethylphenol 5-acetoxy-m-xylene 3-(bromomethyl)-5-methylphenyl acetate 4-(bromomethyl)benzaldehyde

3-(溴甲基)-5-甲基苯基乙酸酯置于三乙酰氧基硼氢化钠,碳酸氢钠,Potassium Carbonate体系中,用 甲醇,水,1,2-二氯乙烷,乙腈 用作溶剂,化学反应 68.0H,反应生成(2R)-1-[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇
参考文献:设计,合成和评估2-氨基噻唑衍生物作为鞘氨醇激酶抑制剂
标题:设计,合成和评估2-氨基噻唑衍生物作为鞘氨醇激酶抑制剂
摘要:鞘氨醇激酶(sphk1,Sphk2)是鞘氨醇-1-磷酸酯(s1P)的主要调节剂,鞘氨醇-1-磷酸酯是一种参与多种生理和病理生理功能的多效脂质介体.Sphk是新型抗癌和抗炎剂的靶标,这些抗癌剂和抗炎剂可促进细胞凋亡并调节自身免疫性疾病.本文中,我们描述了氨基噻唑类sphk抑制剂的设计,合成和评估.通过使用已知的ski-Ii支架进行一系列修饰来定义结构-活性关系,已经发现了有效的抑制剂.我们确定了n-(4-甲基噻唑-2-基)-(2,4'-Bithiazol)-2'-胺(24,St-1803 ; Ic 50 值:7.3μm(sphk1),6.5μm(sphk2))有望成为进一步体内研究和结构开发的有希望的候选者.
Doi:10.1016/j.Bmc.2014.07.044

专利信息

专利号:US-11858953-B2
优先权日:2018-04-04
标 题:Compositions and methods for synthesis of phosphorylated molecules
发明人：CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT
权利人:UNIV CALIFORNIA
摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.

专利号:WO-9102739-A1
优先权日:1989-08-11
标题:Synthesis of glycosides having predetermined stereochemistry
发明人：DANISHEFSKY SAMUEL J
权利人:UNIV YALE
摘要:Methods of stereoselectively preparing a substituted 1,2-anhydrosugar wherein a substituted glycal is converted into a 1,2-anhydrosugar that is utilized to glycosylate a hydroxyl group containing glycal, are disclosed. Methods of preparing a saccharide multimer wherein a nucleophile is reacted with a substituted 1,2-anhydrosugar having a plurality of non-participating substituents, are disclosed. In addition, methods of preparing stereospecific halo-substituted saccharide multimers by haloglycosylation of a glycosyl donor substituted glycal and a glycosyl acceptor glycal derivative in the absence of water and in the presence of a halonium ion, are disclosed. Methods of preparing stereospecific particle-linked halo-substituted saccharide multimers, by haloglycosylation of a particle-linked nucleophilic hydroxyl group with a substituted glycal and a halonium ion, are also disclosed.

专利号:US-10188136-B2
优先权日:2016-02-16
标题:Hydrophobin mimics: process for preparation thereof
发明人：BRITTO Sandanaraj Selvaraj; REDDY Mullapudi Mohan; BHANDARI PAVANKUMAR JANARDHAN; RAO KASULADEVU JAGANNADHA
权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES
摘要:The present invention discloses hydrophobin mimics of formula (I) comprising a protein head group, hydrophilic linker and hydrophobic tail and to a process for synthesis of library of hydrophobin mimics thereof. The hydrophobin mimics of the present invention self-assemble to form protein nanoparticles/nanocontainer either alone or in a specified chemical environment. The hydrophobin mimics (I) of the present invention find application in area of bio-nanotechnology.

专利号:US-7125986-B2
优先权日:1997-12-29
标题:Penicillanic acid derivative compounds and methods of making
发明人：BUYNAK JOHN D; RAO AKIREDDY SRINIVASA; DOPPALAPUDI VENKATA RAMANA
权利人:UNIV SOUTHERN METHODIST
摘要:Compounds of formula I: n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.

专利号:US-7429616-B2
优先权日:2005-07-15
标 题 :Synthesis and complete stereochemical assignment of psymberin/irciniastatin for use as antitumor compounds
发明人：BRABANDER JEF DE; JIANG XIN
权利人:UNIV TEXAS
摘要:The invention relates to the synthesis and complete stereochemical assignments of cytotoxic compounds such as compound 28-a and its stereoisomers: n nThe invention further provides processes for making the compounds, their synthetic intermediates, and for methods of using the compounds and their pharmaceutical compositions for the treatment of neoplastic diseases.

专利号:US-5882901-A
优先权日:1991-06-10
标 题:Modified sialyl Lewisa compounds
发明人：VENOT ANDRE P; NIKRAD PANDURANG V; KASHEM MOHAMMED A
权利人:ALBERTA RES COUNCIL
摘要:The present invention is drawn to methods for the synthesis of Lewis a derivatives modified at the C-2 and/or C-6 position of GlcNAc employing chemo-enzymatic synthesis. The derivatives find use in the treatment and prevention of diseases.