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-7635781-B2 优先权日:2001-05-15 标 题:Synthesis of cyclopentadiene derivatives 发明人:NIFANT EV ILYA; KASHULIN IGOR; IVCHENKO PAVEL; KLUSENER PETER; KORNDORFFER FRANS; DE KLOE KEES; RIJSEMUS JOS 权利人:BASELL POLYOLEFINE GMBH 摘要:A compound of formula (X): n n n n n n n n n n n n wherein n R 1 , R 2 , equal to or different from each other are hydrogen or a linear or branched saturated or unsaturated C 1 -C 20 -alkyl, C 3 -C 20 -cycloalkyl, C 6 -C 20 -aryl, C 7 -C 20 -alkylaryl or C 7 -C 20 -arylalkyl radical, optionally containing heteroatoms belonging to groups 13-17 of the Periodic Table of the Elements; or they can form a C 4 -C 7 ring optionally containing O, S, N, P or Si atoms that can bear substituents; n R 3 is hydrogen or a linear or branched saturated or unsaturated C 1 -C 20 -alkyl, C 3 -C 20 -cycloalkyl, C 6 -C 20 -aryl, C 7 -C 20 -alkylaryl or C 7 -C 20 -arylalkyl radical, optionally containing heteroatoms belonging to groups 13-17 of the Periodic Table of the Elements; or two adjacent R 3 groups can form a C 4 -C 7 ring optionally containing O, S, N, P or Si atoms, wherein said ring can bear substituents; n and at least one of R 1 , R 2 or R 3 is different from hydrogen.
专利号:EP-1926738-B1 优先权日:2005-09-19 标题:Synthesis of cyclopentadienedithiophene derivatives 发明人:GUIDOTTI SIMONA 权利人:BASELL POLYOLEFINE GMBH 摘要:A process for preparing cyclopentadiene derivatives having formula (I) wherein T1 is selected from the group consisting of oxygen (O), or sulphur (S); R1, R2, R3 and R4, are hydrogen atoms, or hydrocarbon radicals; comprising the following steps: a) reacting a compound of formula (II) with a compound of formula (III) in the presence of a palladium or nickel based catalyst and a base; b) contacting the obtained compound with a carbonylating system; and c) treating the product obtained in step b) with a reducing agent.
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-7799524-B2 优先权日:2002-10-03 标 题:Substrates for O6-alkylguanina-DNA alkyltransferase 发明人:KINDERMANN MAIK; JOHNSSON KAI; BIERI CHRISTOPH 权利人:ECOLE POLYTECHNIQUE FERDEALE D 摘要:The invention relates to compounds of formula 1 n nwherein R 1 -R 2 is a guanine derivative; X is oxygen or sulfur; R 3 is a heteroaromatic, unsaturated heterocyclyl or an alkynyl group with the double or triple bond connected to CH 2 ; R 4 is a linker; and L is a label, a plurality of same or different labels, a bond connecting R 4 to R 1 forming a cyclic substrate, or a further group —R 3 —CH 2 —X—R 1 -R 2 . The invention relates also to methods of manufacture of such novel AGT substrates, to intermediates useful in the synthesis of such AGT substrates, and to a method of transferring a label from such AGT substrates to O 6 -alkylguanine-DNA alkyltransferase (AGT) fusion proteins comprising proteins of interest.
专利号:US-5916899-A 优先权日:1996-10-18 标 题:Isoquinoline derivatives and isoquinoline combinatorial libraries 发明人:KIELY JOHN S; GRIFFITH MICHAEL C 权利人:TREGA BIOSCIENCES INC 摘要:The present invention provides the synthesis of heterocyclic compounds based on the isoquinoline ring. More specifically, the invention provides novel isoquinolines as well as novel libraries comprised of many such compounds, and methods of synthesizing the libraries.
[参考文献]: M Lebl, Et Al. New Technique For High-Throughput Synthesis. Bioorg Med Chem Lett. 1999 May 3;9(9):1305-10.
合成参考文献
摘要:Schatz, J.; Seler, M., Science of Synthesis Knowledge Updates, (2011) 2, 408. 摘要:Yerien, D. E.; Barata-Vallejo, S.; Postigo, A., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 9.