专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
专利号:US-6258323-B1 优先权日:1998-11-16 标题:Apparatus and method used in multiple, simultaneous synthesis of general compounds 发明人:HORMANN ROBERT EUGENE; GILBERT DARYL EUGENE; SIOMA EDWARD MICHAEL 权利人:ROHM & HAAS 摘要:The apparatus and method of the present invention provides for conducting simultaneous multiple synthesis of general compounds, which often takes place under varied uneven conditions requiring heating, cooling, agitation, reagent/solvent additions to the reactor contents at each reaction vessel location, supply and maintenance of inert atmosphere and means to facilitate the reflux of the reactor contents. Thus, it becomes necessary to monitor and control the reaction conditions during the simultaneous multiple synthesis of general compounds. The apparatus allows the user to connect various independently controlling and conveying means to each reaction vessel through multiple ports provided on a stopper mounted on each reaction vessel. The apparatus of the present invention permits user to readily access the reaction vessels without interrupting the reactions occurring in the adjacent reaction vessels. The unique geometry and shape of the stopper allows positioning of multiple ports, while still providing the stopper with a compact size. As a result, a large array of reaction vessels can be accommodated in the device of the present invention without significantly increasing the overall size of the apparatus. Some of the general compounds that can be readily synthesized by the apparatus and the method of the present invention include inorganic compounds as well as organic compounds, such as oligomers, polymers, agricultural chemicals, drugs, peptides and oligonucleotides.
专利号:US-6133409-A 优先权日:1996-12-19 标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds 发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F 权利人:AVENTIS PHARM PROD INC 摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
专利号:US-7358372-B2 优先权日:2003-07-31 标 题 :Method for the synthesis of perindopril and the pharmaceutically acceptable salts thereof 发明人:FUGIER CLAUDE; DUBUFFET THIERRY; LANGLOIS PASCAL 权利人:SERVIER LAB 摘要:Process for the synthesis of perindopril of formula (I): n nand its pharmaceutically acceptable salts.
专利号:US-7368580-B2 优先权日:2003-07-31 标 题:Method for the synthesis of perindopril and the pharmaceutically acceptable salts thereof 发明人:FUGIER CLAUDE; DUBUFFET THIERRY; LANGLOIS PASCAL 权利人:SERVIER LAB 摘要:Process for the synthesis of perindopril of formula (I): n nand its pharmaceutically acceptable salts.
专利号:US-7973173-B2 优先权日:2005-07-05 标 题:Process for the synthesis of an ACE inhibitor 发明人:KANKAN RAJENDRA NARAYANRAO; RAO DHARMARAJ RAMACHANDRA; PHULL MANJINDER SINGH; SAWANT ASHWINI; BIRARI DILIP RAMDAS 权利人:CIPLA LTD 摘要:A process for the synthesis of trandolapril which comprises condensing N—[I—(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride with trans octahydro-1H-indole-2-carboxylic acid in a first organic solvent comprising a water immiscible inert organic solvent and in the presence of a base, and isolating trandolapril from a second organic solvent. N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride may also be condensed with (2S,3aR,7aS) octahydro-1H-indole-2-carboxylic acid in a first organic solvent and in the presence of a base, and trandolapril isolated. There is also provided a process for the resolution of racemic trans octahydro-1H-indole-2-carboxylc acid.
[参考文献]: 2-Indolecarboxylic Acid. [参考文献]: J E Huettner, Et Al. Indole-2-Carboxylic Acid: A Competitive Antagonist Of Potentiation By Glycine At The Nmda Receptor. Science. 1989 Mar 24;243(4898):1611-3. [参考文献]: Adelle A Vandersteen, Et Al. Protonated Carbonic Acid And Reactive Intermediates In The Acidic Decarboxylation Of Indolecarboxylic Acids. J Org Chem. 2012 Aug 3;77(15):6505-9. [参考文献]: Chandrasekaran Praveen, Et Al. Gold(Iii) Chloride Catalyzed Regioselective Synthesis Of Pyrano[参考文献]: Gamze Bora-Tatar, Et Al. Molecular Modifications On Carboxylic Acid Derivatives As Potent Histone Deacetylase Inhibitors: Activity And Docking Studies. Bioorg Med Chem. 2009 Jul 15;17(14):5219-28.
合成参考文献
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 51. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 87. 摘要:Harris, P. A., Science of Synthesis Knowledge Updates, (2021) 3, 172. 摘要:Hapiot, F.; Monflier, E., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 782. 摘要:Stewart, S. G., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 442.