CAS: 864754-13-2; Tert-Butyl 4-(4-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)Benzoyl)Piperazine-1-Carboxylate

上下游产品

4-carboxyphenylboronic acid pinacol ester 1-t-Butoxycarbonylpiperazine tert-butyl 4-(4-iodobenzoyl)piperazine-1-carboxylate bis(pinacol)diborane 4-{4-[3-(4-carbamoyl-phenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-benzoyl}-piperazine-1-carboxylic acid tert-butyl ester tert-Butyl 4-(4-(5-amino-6-(oxazolo[4,5-c]pyridin-2-yl)pyrazin-2-yl)benzoyl)piperazine-1-carboxylate

频哪醇置于1-羟基苯并三唑,三乙胺体系中,用 乙酸乙酯,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 52.0H,反应生成 4-(4-Boc-哌嗪-1-羰基) 苯硼酸频哪酯
参考文献:Identification Of New γ-Hydroxybutenolides That Preferentially Inhibit The Activity Of Mpges-1
标题:Identification Of New γ-Hydroxybutenolides That Preferentially Inhibit The Activity Of Mpges-1
摘要:Microsomal Prostaglandin E-2 Synthase-1 (Mpges-1) Has Been Recognized As Novel,Promising Drug Target For Anti-Inflammatory And Anticancer Drugs. Mpges-1 Catalyzes The Synthesis Of The Inducible Prostaglandin E-2 In Response To Pro-Inflammatory Stimuli,Rendering This Enzyme Extremely Interesting In Drug Discovery Process Owing To The Drastic Reduction Of The Severe Side Effects Typical For Traditional Non-Steroidal Anti-Inflammatory Drugs. In The Course Of Our Investigations Focused On This Topic,We Identified Two Interesting Molecules Bearing The Gamma-Hydroxybutenolide Scaffold Which Potently Inhibit The Activity Of Mpges-1. Notably,The Lead Compound 2C That Inhibited Mpges-1 With Ic50 = 0.9 Mu M,Did Not Affect Other Related Enzymes Within The Arachidonic Acid Cascade. (C) 2012 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2012.06.032

专利信息

专利号:US-7465842-B2
优先权日:2004-08-26
标 题 :Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermediates
发明人：KUNG PEI-PEI; MARTINEZ CARLOS; TAO JUNHUA
权利人:AGOURON PHARMA
摘要:The invention relates to biocatalytic methods for preparing enantiomerically pure stereoisomers of 1-(2,6-dichloro-3-fluorophenyl)ethanol. Disclosed are methods of preparation of the desired (S)-enantiomer, which methods are based on a combination of enzymatic resolution, chemical esterification and chemical hydrolysis with inversion of 1-(2,6-dichloro-3-fluorophenyl)ethyl esters or stereoselective bio-reduction of 2,6-dichloro-3-fluoro-acetophenone with a biocatalyst such as an enzyme or a microorganism. The chiral (S)-enantiomer can be used in the synthesis of certain enantiomerically enriched, ether linked 2-aminopyridine compounds that potently inhibit auto-phosphorylation of human heptocyte growth factor receptor.

专利号:US-10995078-B2
优先权日:2013-03-13
标 题:Compounds and compositions for inhibition of FASN
发明人：BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J
权利人:FORMA THERAPEUTICS INC
摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:

专利号:US-9938258-B2
优先权日:2012-11-29
标 题:Substituted 2,3-dihydrobenzofuranyl compounds and uses thereof
发明人：BALOGLU ERKAN; SHECHTER SHARON; SHACHAM SHARON; MCCAULEY DILARA; SENAPEDIS WILLIAM; GOLAN GALI; KALID ORI
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to substituted 2,3-dihydrobenzofuranyl compounds, and more particularly to a compound represented by Structural Formula I: n nor a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.

专利号:US-8592448-B2
优先权日:2008-11-20
标题:Substituted pyrrolo[2,3-b]-pyridines and -pyrazines
发明人：CHEN XIN; JIN MELZHONG; KLEINBERG ANDREW; LI AN-HU; MULVIHILL MARK J; STEINIG ARNO G; WANG JING
权利人:CHEN XIN; JIN MELZHONG; KLEINBERG ANDREW; LI AN-HU; MULVIHILL MARK J; STEINIG ARNO G; WANG JING; OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met.