卡马西平置于乙醇碲体系中,用 四氯化碳 用作溶剂,化学反应 3.0H,以85%的收率获得亚氨基芪 参考文献:Chemoselective Reactions Of Tellurium Tetraethoxide Towards Thioamides And Amides 标题:Chemoselective Reactions Of Tellurium Tetraethoxide Towards Thioamides And Amides 摘要:四乙氧基碲在室温下与伯硫酰胺反应,高效生成腈.另一方面,四乙氧基碲与酰胺的反应很大程度上依赖于温度,在80oc主要生成酯,而在更高温度下生成腈.同样,四乙氧基碲容易引发尿素中的c-N键断裂,生成氨基甲酸酯和胺. Doi:10.1246/bcsj.67.1759
专利号:WO-9517903-A1 优先权日:1993-12-28 标 题:Modular design and synthesis of oxazolone-derived molecules 发明人:HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.
专利号:US-10414903-B2 优先权日:2016-11-11 标题 :Methods for synthesis of end-functionalized polyolefins 发明人:GUIRONNET DAMIEN S; HYATT MICHAEL G; WALSH DYLAN J 权利人:UNIV ILLINOIS 摘要:A strategy for the synthesis of semi-telechelic polyethylene through the palladium diimine-catalyzed chain transfer polymerization of ethylene using various silanes as chain transfer agents is reported. Polymer molecular weight and end-group chemical structure can be tuned by varying the chain transfer agent as well as its concentration. NMR spectroscopy confirms that the silicon of the chain transfer agent is incorporated into the polymer. The stability of the catalyst toward polar monomer enables the chain transfer polymerization of semi-telechelic poly(ethylene-methyl acrylate) copolymers.
专利号:WO-2018217538-A1 优先权日:2017-05-23 标题 :Synthesis of substituted acridines 发明人:FORT ERIC H; JAYE JOSEPH A; MCCORMICK GRANT M; BERGER KRISTEN E 权利人:UNIV OF ST THOMAS 摘要:Disclosed is a method of making substituted acridines. The method includes the step of reacting a bis(halophenyl) amine with an alkyne for a time and at a temperature to yield a substituted acridine.
专利号:US-6225329-B1 优先权日:1998-03-12 标 题 :Modulators of protein tyrosine phosphatases (PTPases) 发明人:RICHTER LUTZ STEFAN; ANDERSEN HENRIK SUNE; VAGNER JOSEF; JEPPESEN CLAUS BEKKER; MOELLER NIELS PETER HUNDAHL; BRANNER SVEN; SU JING; BAKIR FARID; JUDGE LUKE MILBURN 权利人:NOVO NORDISK AS 摘要:The present invention provides novel compounds of Formula 1, compositions containing these compounds, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like, n wherein A, R 1 , R 2 , R 3 , R 4 , R 16 and R 17 are as defined in the specification. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
专利号:US-2005119332-A1 优先权日:1998-03-12 标 题 :Substituted thiophene compounds as modulators of protein tyrosine phosphatases (PTPases) 发明人:JEPPESEN LONE; ANDERSEN HENRIK S; OLSEN OLE H; JUDGE LUKE M; HOLSWORTH DANIEL D; BAKIR FARID; AXE FRANK U; GE YU 摘要:The present invention provides novel compounds of formula 1a, n nnovel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
专利号:US-9388147-B2 优先权日:2009-11-13 标题 :Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TIMONY GREGG ALAN; BROOKS JENNIFER L; PEACH ROBERT; SCOTT FIONA LORRAINE; HANSON MICHAEL ALLEN 权利人:RECEPTOS INC; CELGENE INTERNAT II SÃ?RL 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
[参考文献]: Christian P, Et Al. Crystallization Of Carbamazepine In Proximity To Its Precursor Iminostilbene And A Silica Surface. Cryst Growth Des. 2016 May 4;16(5):2771-2778. Epub 2016 Mar 30. [参考文献]: H Vijay Kumar, Et Al. Synthesis And Antioxidant Properties Of Some Novel 5H-Dibenz[参考文献]: Olivier Mathieu, Et Al. Effects Of Carbamazepine And Metabolites On Il-2, Il-5, Il-6, Il-10 And Ifn-γ Secretion In Epileptic Patients: The Influence Of Co-Medication. Pharmacol Rep. 2011;63(1):86-94. [参考文献]: Predrag Lj Dzodi, Et Al. Determination Of Carbamazepine And Its Impurities Iminostilbene And Iminodibenzyl In Solid Dosage Form By Column High-Performance Liquid Chromatography. J Aoac Int. 2010 Jul-Aug;93(4):1059-68. [参考文献]: S M Furst, Et Al. Carbamazepine Metabolism To A Reactive Intermediate By The Myeloperoxidase System Of Activated Neutrophils. Biochem Pharmacol. 1993 Mar 24;45(6):1267-75.
合成参考文献
摘要:Camp, J. E., Science of Synthesis Knowledge Updates, (2012) 1, 342. 摘要:Camp, J. E., Science of Synthesis Knowledge Updates, (2012) 1, 342. 摘要:Camp, J. E., Science of Synthesis Knowledge Updates, (2012) 1, 344. 摘要:Camp, J. E., Science of Synthesis Knowledge Updates, (2012) 1, 347. 摘要:Camp, J. E., Science of Synthesis Knowledge Updates, (2012) 1, 340.