219611-74-2 = 1875-48-5 + 90564-77-5 反应条件:1.1 Reagents: Hydrazine Hydrate (1:1) Solvents: Ethanol,Water; Rt; 5 H,Reflux; Overnight,4 °C 标题:Synthesis And Cytotoxic Activity Of (4-Substituted-Benzylidene)-(3-Phenyl-1,2,4-Oxadiazol-5-Yl)Methylamines 作者:Kucukoglu,K.; Tugrak,M.; Demirtas,A.; Sakagami,H.; Gul,H. I. 参考文献:Pharmaceutical Chemistry Journal 日期:2016 卷标:50(4) 页码:234-238
1,4-二氧六环置于palladium On Activated Charcoal体系中,用 溶剂黄146 用作溶剂,化学反应生成氨基邻苯二甲胺 参考文献:Method Of Inhibiting Binding Of Nerve Growth Factor To P75 Ntr Receptor 标题:Method Of Inhibiting Binding Of Nerve Growth Factor To P75 Ntr Receptor 摘要:本发明涉及抑制神经生长因子与p75Ntr共同神经营养因子受体结合的组合物和使用方法.在一个实施例中,抑制神经生长因子与p75Ntr结合的化合物,特别是当与神经生长因子结合时,至少包括以下两种:(1)第一个电负原子或功能基团,位于与神经生长因子的lys34相互作用的位置;(2)第二个电负原子或功能基团,位于与神经生长因子的lys95相互作用的位置;(3)第三个电负原子或功能基团,位于与神经生长因子的lys88相互作用的位置;(4)第四个电负原子或功能基团,位于与神经生长因子的lys32相互作用的位置;以及(5)与神经生长因子的ile31,Phe101和phe86形成的疏水区域相互作用的疏水基团.
专利号:WO-9616071-A1 优先权日:1994-11-21 标题:PROCESSES FOR THE SYNTHESIS OF 3'-SUBSTITUTED LEWISx COMPOUNDS 发明人:SRIVASTAVA OM; IPPOLITO ROBERT; SRIVASTAVA GEETA; SZWEDA ROMAN; OHUCHI TOSHIO 权利人:GLYCOMED INC; SRIVASTAVA OM; IPPOLITO ROBERT; SRIVASTAVA GEETA; SZWEDA ROMAN; OHUCHI TOSHIO 摘要:Disclosed are processes for the chemical synthesis of 3'-substituted Lewis-OR compounds where R is an aglycon of at least one carbon atom. One particular compound prepared by the processes of this invention is 8-methoxycarbonyl-octyl-2-acetamido-3-O-( alpha -L-fucopyranosyl)-4-O-[3-O-sulfo- beta -D-galactopyranosyl]-2-deoxy- beta -D-glucopyranoside.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-8604241-B2 优先权日:2009-01-29 标题:Method for synthesis of (1S, 2R)-milnacipran 发明人:NICOLAS MARC; HELLIER PAUL; DIARD CATHERINE; SUBRA LAURENT 权利人:NICOLAS MARC; HELLIER PAUL; DIARD CATHERINE; SUBRA LAURENT; PF MEDICAMENT 摘要:The present invention relates to a method for synthesizing a pharmaceutically acceptable acid addition salt of (1S, 2R)-milnacipran comprising the following successive steps: (a) reaction of phenylacetonitrile and of (R)-epichlorhydrin in the presence of a base containing an alkaline metal, followed by a basic treatment, and then by an acid treatment in order to obtain a lactone; (b) reaction of said lactone with MNEt 2 , wherein M represents an alkaline metal, or with NHEt 2 in the presence of a Lewis acid-amine complex, in order to obtain an amide-alcohol; (c) reaction of said amide-alcohol with thionyl chloride in order to obtain a chlorinated amide; (d) reaction of said chlorinated amide with a phthalimide salt in order to obtain a phthalimide derivative; (e) hydrolysis of the phthalimide group of said phthalimide derivative in order to obtain (1S, 2R)-milnacipran, and (f) salification of (1S, 2R)-milnacipran in a suitable solvent system in the presence of a pharmaceutically acceptable acid.
专利号:US-2006111438-A1 优先权日:2004-10-21 标 题:Asymmetric synthesis of substituted dihydrobenzofurans 发明人:GONTCHAROV ALEXANDER V; KHAFIZOVA GULNAZ; POTOSKI JOHN R; YU QING; SHAW CHIA-CHENG; STACK GARY P; ZHOU DAHUI 权利人:WYETH CORP 摘要:The present invention concerns production of a compound of the formula n n nor a pharmaceutically acceptable salt thereof by a process which utilizes the cyclization of a compound of the formula: n n nwhere Ar, Y, R 1 , R y , R 2 , and m are as defined herein.
专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-8461298-B2 优先权日:2004-11-01 标 题:Compositions and methods for modification of biomolecules 发明人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL 权利人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; UNIV CALIFORNIA 摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
[参考文献]: Kung-Shou Yang, Et Al. Enantioselective Aziridination Of Alkenes With N-Aminophthalimide In The Presence Of Lead Tetraacetate-Mediated Chiral Ligand. Org Lett. 2002 Apr 4;4(7):1107-9.
合成参考文献
摘要:Aggarwal, P.; Bebbington, M. W. P., Science of Synthesis Knowledge Updates, (2012) 2, 378. 摘要:Muchalski, H.; Johnston, J. N., Science of Synthesis: Stereoselective Synthesis, (2011) 1, 159. 摘要:Muchalski, H.; Johnston, J. N., Science of Synthesis: Stereoselective Synthesis, (2011) 1, 155.