2,6-二甲基吡啶置于manganese(Iv) Oxide,2,2,2-三氟苯乙酮,双氧水,Potassium Carbonate,乙腈,三氟乙酸酐体系中,用 二氯甲烷,水,1,2-二氯乙烷,叔丁醇 用作溶剂,化学反应 98.0H,反应生成6-甲基-2-吡啶甲醛 参考文献:Methyl Scanning And Revised Binding Mode Of 2-Pralidoxime,An Antidote For Nerve Agent Poisoning 标题:Methyl Scanning And Revised Binding Mode Of 2-Pralidoxime,An Antidote For Nerve Agent Poisoning 摘要:Organophosphorus Nerve Agents (Opnas) Inhibit Acetylcholinesterase (Ache) And,Despite The Chemical Weapons Convention Arms Control Treaty,Continue To Represent A Threat To Both Military Personnel And Civilians. 2-Pralidoxime (2-Pam) Is Currently The Only Therapeutic Countermeasure Approved By The United States Food And Drug Administration For Treating Opna Poisoning. However,2-Pam Is Not Centrally Active Due To Its Hydrophilicity And Resulting Poor Blood-Brain Barrier Permeability; Hence,These Deficiencies Warrant The Development Of More Hydrophobic Analogs. Specifically,Gaps Exist In Previously Published Structure Activity Relationship (Sar) Studies For 2-Pam,Thereby Making It Difficult To Rationally Design Novel Analogs That Are Concomitantly More Permeable And More Efficacious. In This Study,We Methodically Performed A Methyl Scan On The Core Pyridinium Of 2-Pam To Identify Ring Positions That Could Tolerate Both Additional Steric Bulk And Hydrophobicity. Subsequently,Sar-Guided Molecular Docking Was Used To Rationalize Hydropathically Feasible Binding Modes For 2-Pam And The Reported Derivatives. Overall,The Data Presented Herein Provide New Insights That May Facilitate The Rational Design Of More Efficacious 2-Pam Analogs. Doi:10.1021/acsmedchemlett.9B00586
专利号:US-6121054-A 优先权日:1997-11-19 标 题 :Method for separation of liquid and solid phases for solid phase organic syntheses 发明人:LEBL MICHAL 权利人:TREGA BIOSCIENCES INC 摘要:A simple, efficient apparatus and method for separation of solid and liquid phases useful in methods of high-throughput combinatorial organic synthesis of large libraries or megaarrays of organic compounds is disclosed. The apparatus and method are useful, whether as part of an automated, robotic or manual system for combinatorial organic synthesis. In a preferred embodiment, an apparatus and method of removal of liquid phase from solid phase compatible with microtiter plate type array(s) of reaction vessels is disclosed.
专利号:US-5783577-A 优先权日:1995-09-15 标题 :Synthesis of quinazolinone libraries and derivatives thereof 发明人:HOUGHTEN RICHARD A; OSTRESH JOHN M 权利人:TREGA BIOSCIENCES INC 摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.
专利号:WO-9710221-A1 优先权日:1995-09-15 标 题:Synthesis of quinazolinone libraries 发明人:HOUGHTEN RICHARD A; OSTRESH JOHN M 权利人:TORREY PINES INST 摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.
专利号:US-6045755-A 优先权日:1997-03-10 标题 :Apparatus and method for combinatorial chemistry synthesis 发明人:LEBL MICHAEL; POKORNY VIT; KRCHNAK VIKTOR 权利人:TREGA BIOSCIENCES INC 摘要:In a first embodiment, this invention includes an integrated robot apparatus for performing combinatorial chemistry synthesis protocols and having interchangeable work-stations, robot arm tools, and reaction vessels and reaction vessel arrays. The work-stations and tools are specialized to perform tasks necessary for the synthesis in a plurality of the reaction vessels grouped in a plurality of the reaction vessel arrays. Preferably, these elements function interchangeably because they have standardized sizes and conformation. The work-stations and tools include those for fluid dispensing or aspirating from individual reaction vessels or from all the reaction vessels in an array simultaneously. The reaction vessels can include, alternatively, stackable, ball-sealed reaction vessels, microtitre-like reaction vessel arrays, arrays of independent reaction vessels, valve-sealed reaction vessels, septum-sealed reaction vessels, and syringe reaction vessels. In alternative embodiments, this invention includes these work-stations, tools, reaction vessels and reaction vessel arrays in various combinations or sub-combinations either for use in partially integrated robots or for manual or standalone use.
专利号:US-8962839-B2 优先权日:2010-11-19 标题:Chiral spiro-pyridylamidophosphine ligand compound, synthesis method therefor and application thereof 发明人:ZHOU QILIN; XIE JIANHUA; LIU XIAOYAN; XIE JIANBO; WANG LIXIN 权利人:ZHOU QILIN; XIE JIANHUA; LIU XIAOYAN; XIE JIANBO; WANG LIXIN; ZHEJIANG JIUZHOU PHARMA SCIENCE & TECHNOLOGY CO LTD 摘要:The present invention relates to a chiral spiro-pyridylamidophosphine ligand compound, synthesis method therefor and application thereof. The chiral spiro-pyridylamidophosphine compound is a compound having a structure of Formula (I), a racemate or optical isomer thereof, or a catalytically acceptable salt thereof, and is mainly characterized by having a chiral spiro-dihydro-indene skeleton in its structure. The chiral spiro-pyridylamidophosphine compound may be synthesized with optical active 7-diaryl/alkylphosphino-7′-amino-1,1′-spiro-dihydro-indene or substituted 7-diaryl/alkylphosphino-7′-amino-1,1′-spiro-dihydro-indene having a spiro-skeleton as chiral starting material. The chiral spiro-pyridylamidophosphine compound may be used as a chiral ligand in asymmetric hydrogenation of a carbonyl compound catalyzed by iridium, in which the reaction activity is very high, the amount of the catalyst may be 0.0001 mol %, and the enantioselectivity of the reaction is up to 99.9% ee.
专利号:US-7071290-B2 优先权日:2001-03-13 标题 :Polymers and oligomers, their synthesis, and electronic devices incorporating same 发明人:EPSTEIN ARTHUR J; WANG DAIKE 权利人:UNIV OHIO STATE 摘要:The invention relates to polymers and oligomers, methods of their synthesis, and electronic devices comprising them.