专利号:US-9388131-B2 优先权日:2011-04-27 标题:Automated synthesis of small molecules using chiral, non-racemic boronates 发明人:BURKE MARTIN D; LI JUNQI; GILLIS ERIC P 权利人:UNIV ILLINOIS 摘要:Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.
专利号:US-7692019-B2 优先权日:2000-12-04 标 题:Methods for the stereoselective synthesis of substituted piperidines 发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HEFFERNAN MICHELE L R; HOEMANN MICHAEL Z; KESSLER DONALD W; SHAO LIMING; WU XINHE; XIE ROGER L 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.
专利号:US-8334381-B2 优先权日:2006-11-16 标题 :Process for the preparation of intermediates useful in the synthesis of imatinib 发明人:FALCHI ALESSANDRO; GRENDELE ENNIO; MOTTERLE RICCARDO; STIVANELLO MARIANO 权利人:FALCHI ALESSANDRO; GRENDELE ENNIO; MOTTERLE RICCARDO; STIVANELLO MARIANO; ITALIANA SINT SPA 摘要:It is the object of the present invention a process for the preparation of 4-methyl-N3-[4-(3-pyridinyl)-2-pyrimidinyl]-1,3-benzenediamine and analogues thereof, intermediates useful for the synthesis of Imatinib, or 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide.
专利号:WO-2012088402-A1 优先权日:2010-12-22 标题 :Synthesis of conolidine and discovery of a potent non-opioid analgesic for pain 发明人:BOHN LAURA M; MICALIZIO GLENN C 权利人:SCRIPPS RESEARCH INST; BOHN LAURA M; MICALIZIO GLENN C 摘要:The first de novo synthetic pathway to the exceptionally rare C5-nor stemmadenine natural product, conolidine, and the first asymmetric synthesis of any member of this natural product class arc described. C5-nor stemmadenine compositions are also described. These compounds, for example,(+/- )-,(+)- and (-)-conolidine are potent and efficacious non-opioid analgesics in tonic and persistent pain.
专利号:US-6413957-B1 优先权日:1998-04-21 标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SUIBB PHARMA COM 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-8728750-B2 优先权日:2006-09-06 标 题 :Process for preparation of optically active N-protected 3-aminopyrrolidine or optically active N-protected 3-aminopiperidine and the corresponding ketones by optical resolution of the racemic amine mixtures employing a bacterial omega-transaminase 发明人:ROBINS KAREN; BORNSCHEUER UWE; HÖHNE MATTHIAS 权利人:ROBINS KAREN; BORNSCHEUER UWE; HÖHNE MATTHIAS; LONZA AG 摘要:The present invention relates to the production of optically active amines, which can be used as intermediate products in a synthesis of for instance pharmaceutical products.
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合成参考文献
摘要:Matsunaga, S., Science of Synthesis Knowledge Updates, (2010) 4, 219. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 251. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 33. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 171. 摘要:Singh, F. V., Science of Synthesis Knowledge Updates, (2021) 1, 154.