专利号:EP-2280974-B1 优先权日:2008-04-30 标题:Stereoselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:REEVES JONATHAN TIMOTHY; SONG JINHUA J; TAN ZHULIN 权利人:BOEHRINGER INGELHEIM INT; BOEHRINGER INGELHEIM PHARMA 摘要:A process for stereoselective synthesis of a compound of Formula (I) wherein R1, R2, R3, R4, and R5 are as described herein.
专利号:US-7112700-B1 优先权日:2005-04-14 标 题 :Efficient and economic asymmetric synthesis of nootkatone, tetrahydronootkatone, their precursors and derivatives 发明人:SAUER ANNE M; CROWE WILLIAM E; LAINE ROGER A; HENDERSON GREGG 权利人:UNIV LOUISIANA STATE 摘要:An inexpensive, stereoselective synthesis for nootkatone, tetrahydronootkatone, and their derivatives is disclosed. The starting materials used in the synthesis are inexpensive. The principal starting material, (−)-β-Pinene, is on the GRAS list (generally recognized as safe).
专利号:US-6051704-A 优先权日:1996-07-22 标题:Synthesis of macrocyclic tetraamido-N ligands 发明人:GORDON-WYLIE SCOTT W; COLLINS TERRENCE J 权利人:UNIV CARNEGIE MELLON 摘要:New synthetic methods for the preparation of macrocyclic amido-N donor ligands are provided. The primary method of the present invention involves in general only two synthetic steps. In the first step, an α or β amino carboxylic acid is allowed to react with an optimal (approximately stoichiometric) amount of an activated malonate or oxalate derivative with mild heating. Upon completion of the double coupling reaction, hydrolysis of the reaction mixture yields a diamide containing intermediate (a macro linker). In the second step, stoichiometric amounts of a diamine, preferably an orthophenylene diamine, are added to the macro linker intermediate in the presence of a coupling agent and heat. This second double coupling reaction, is allowed to proceed for a period of time sufficient to produce a macrocyclic tetraamido compound. The substituent groups on the α or β amino carboxylic acid, the malonate, and the aryl diamine may all be selectively varied so that the resulting tetraamido macrocycle can be tailored to specific desired end uses. The macrocyclic tetraamide ligand may then be complexed with a metal, such as a transition metal, and preferably the middle and later transition metals, to form a robust chelate complex suitable for catalyzing oxidation reactions.
专利号:US-7060818-B2 优先权日:2003-02-21 标题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process 发明人:HORWITZ COLIN P; GHOSH ANINDYA 权利人:UNIV CARNEGIE MELLON 摘要:An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate. Following deprotection, the diamide diamine intermediate is reacted with an activated diacid, such as an activated malonate, oxalate or succinate derivative to form the macrocyclic tetraamido compound. The macrocyclic tetraamido compound may further be complexed with a transition metal.
专利号:US-10836777-B2 优先权日:2016-12-30 标 题:Method for preparing 2-(cyclohexenylidene) malonic acid derivatives and uses thereof 发明人:SUN YINWEI; WANG ZHONGYUAN; ZHANG PAN; CHEN BANGCHI 权利人:ORIENTAL LUZHOU AGROCHEMICALS CO LTD 摘要:Disclosed are a method for preparing 2-(cyclohexenylidene) malonic acid derivatives and uses thereof. In this method, an olefin and a 2-substituted malonic acid derivative are used as starting materials to prepare the 2-(cyclohexenylidene) malonic acid derivative in the presence of a catalyst through cyclization reaction. This method has the following advantages: (1) the method can be very efficiently used for the synthesis of highly sterically-hindered 2-(2,6-disubstituted cyclohexenylidene) malonic acid derivatives; (2) the reaction yield is high, the reaction conditions are mild, and the wastes are less, favorable for industrial production. More importantly, the present invention extends the further use of 2-(cyclohexenylidene)malonic acid derivatives in organic synthesis, especially in the synthesis of 2-aryl malonic acid derivatives and their corresponding drugs such as Pinoxaden.
专利号:US-7323589-B2 优先权日:2000-10-26 标 题:Intermediates for use in retinoid synthesis 发明人:VALLA ALAIN; CARTIER DOMINIQUE; LABIA ROGER; POTIER PIERRE JEAN-PAUL 权利人:CENTRE NAT RECH SCIENT 摘要:The invention concerns compounds of formula (1) wherein in particular G represents the —N(CH 3 ) 2 —, —N(C 2 H 5 ) 2 -group or N-pyrrolidine: n is an integer equal to 1 or 2: R 1 , R 2 and R 3 , independently of one another, represent a hydrogen atom or a methyl group, the successive unsaturated units capable of being moreover identical or different, provided that at least one of the substituents R 1 , R 2 and R 3 is different from H: and Y 1 and Y 2 represent each a —COOCH 3 group or a COOC 2 H 5 group.
参考标题:Synthesis Of Nitrogen Heterocycles Via α-Aminoalkyl Radicals Generated From α-Silyl Secondary Amines Under Visible Light Irradiation 作者:Kazunari Nakajima,Mai Kitagawa,Yuya Ashida,Yoshihiro Miyake,Yoshiaki Nishibayashi 摘要:We Have Succeeded In The Visible Light-Mediated Synthetic Use Of α-Aminoalkyl Radicals Derived From α-Silyl Secondary Amines Toward Addition To α,β-Unsaturated Carbonyl Compounds. The Resulting γ-Aminocarbonyl Compounds Are Converted Into γ-Lactams And Pyrroles In A One-Pot Process.
合成参考文献
摘要:Chessum, N.; Couty, S.; Jones, K., Science of Synthesis, (2009) 48, 293.