专利号:WO-2014011120-A1 优先权日:2012-07-13 标 题 :Endoperoxides, synthesis and uses thereof for the treatment of neoplastic diseases such as cancer 发明人:TAN NGUAN SOON; CHIBA SHUNSUKE 权利人:UNIV NANYANG TECH 摘要:The present invention generally relates to processes and methods for the synthesis of endoperoxide compounds. More specifically, the invention relates to a method for preparing endoperoxide compounds starting from an aryl imine of formula (I) in the presence of a metallic catalyst and oxygen. The present invention also relates to endoperoxide compounds of formula (III) and their pharmaceutically acceptable salts thereof, useful for therapy. All substituents are defined herein. Also disclosed are methods of treating cancer using the compounds of formula (III).
专利号:US-6362009-B1 优先权日:1997-11-21 标 题 :Solid phase synthesis of heterocycles 发明人:MUNOZ BENITO; CHEN CHIXU 权利人:MERCK & CO INC 摘要:Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.
专利号:US-6340751-B1 优先权日:1998-07-24 标 题 :Process for the preparation of 4-substituted azetidinone derivatives 发明人:SAITO TAKAO; MURAYAMA TOSHIYUKI; MATSUMOTO TAKAJI; MIURA TAKASHI 权利人:TAKASAGO PERFUMERY CO LTD 摘要:Disclosed is a process for the preparation of a 4-substituted azetidinone derivative, which comprises reacting an azetidinone derivative and an amide compound in the presence of a magnesium compound such as those represented by the following formulas (II): n and (IV): n represented by the following formula (III): n n n MgR 5 R 6   (III) n n n wherein R 5 represents a C 1-12 alkyl group, a C 2-5 alkenyl group, a 5- to 8-membered alicyclic group which may be substituted by a lower C 1-4 alkyl group, a phenyl group which may be substituted by a lower C 1-4 alkyl group, a lower C 1-4 alkoxy group or a halogen atom or a benzyl group which may be substituted by a lower C 1-4 alkyl group, a lower C 1-4 alkoxy group or a halogen atom, and R 6 represents a halogen atom, a methanesulfonyloxy group, a benzenesulfonyloxy group, a p-toluenesulfonyloxy group, a trifluoromethanesulfonyloxy group, an acetoxy group which may be substituted by a halogen atom or a cyano group or an OR 7 group (R 7 representing a lower C 1-4 alkyl group, a substituted or unsubstituted phenyl group or a substituted or unsubstituted benzyl group). The process provides an industrially excellent process for the preparation of a 4-substituted azetidinone derivative which permits the selective preparation of an intermediate for the synthesis of a carbapenem antibacterial agent having a desired 1-β′ configuration.
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:US-4246176-A 优先权日:1979-07-05 标 题 :Synthesis of 5-aroyl-1-hydrocarbylpyrrole-2-acetic acid 发明人:ZAIKO EDWARD J 权利人:ETHYL CORP 摘要:The reaction between a 5-cyano-1-hydrocarbylpyrrole-2-acetic acid and an aryl Grignard compound to produce a ketimine salt-containing reaction intermediate is improved by performing such reaction in an aromatic ether reaction medium at a temperature above about 100° C. As compared to the previously known process, the reaction rate is markedly increased without loss of selectivity. Also, the water insolubility of aromatic ethers simplifies product work-up and recovery, reduces product losses, and facilitates solvent recovery and recycle. Preferably, the aryl Grignard reagent is prepared at the outset in tetrahydrofuran or methyl tetrahydrofuran--solvents in which such Grignard reagents are readily and safely produced. The resultant Grignard solution may then be employed in forming the aromatic ether-containing reaction medium in which the above reaction is conducted.
专利号:US-9243004-B2 优先权日:2011-07-22 标题 :Synthesis of boronic esters and boronic acids using grignard reagents 发明人:CLARY JACOB W; SINGARAM BAKTHAN 权利人:CLARY JACOB W; SINGARAM BAKTHAN; UNIV CALIFORNIA 摘要:Boronic esters and boronic acids are synthesized at ambient temperature in an ethereal solvent by the reaction of Grignard reagents with a boron-containing substrate. The boron-containing substrate may be a boronic ester such as pinacolborane, neopentylglycolborane, or a dialkylaminoborane compound such as diisopropylaminoborane. The Grignard reagents may be pre-formed or generated from an alkyl, alkenyl, aryl, arylalkyl, heteroaryl, vinyl, or allyl halide compound and Mg 0 . When the boron-containing substrate is a boronic ester, the reactions generally proceed at room temperature without added base in about 1 to 3 hours to form a boronic ester compound. When the boron-containing substrate is a dialkylaminoborane compound, the reactions generally proceed to completion at 0° C. in about 1 hour to form a boronic acid compound.
参考标题:Synthesis And Biological Activity Of Substituted 2,4-Diaminopyrimidines That Inhibit Bacillus Anthracis 作者:Baskar Nammalwar,Richard A. Bunce,K. Darrell Berlin,Christina R. Bourne,Philip C. Bourne,Esther W. Barrow,William W. Barrow |发布日期:2012.8 摘要:The Lowest Mics With Values Of 0.5 μg/ml And 0.375-1.5 μg/ml, Respectively. It Is Likely That The S Isomers Of 1 Will Bind The Substrate-Binding Pocket Of Dihydrofolate Reductase (Dhfr) As In B. Anthracis Was Found For (S)-1A. The Final Step In The Convergent Synthesis Of Target Systems 1 From (+/-)-1-(1-Substituted-2(1H)-Phthalazinyl)-2-Propen-1-Ones 6 With 2,4-Diamino-5-(5-Iodo-3,4-Dimethoxybenzyl)Pyrimidine
合成参考文献
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