专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
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-6187923-B1 优先权日:1998-11-09 标题 :Process for the synthesis of quinazolinones 发明人:DENER JEFFREY MARK; LY CUONG QUOC 权利人:AXYS ADVANCED TECHNOLOGIES INC 摘要:The present invention provides a process for synthesizing a compound or a library of compounds of Formula 1A and 1B:
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-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.
专利号:WO-0053313-A2 优先权日:1999-03-09 标 题:Lanthanide catalysts for synthesis of compounds and combinatorial 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:Barsegyan, Y. A.; Vil’, V. A.; Tomkinson, N. C. O.; Terent’ev, A. O., Science of Synthesis Knowledge Updates, (2022) 1, 239. 摘要:Ciszek, B.; Fleischer, I., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 2, 164.