专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:US-2005019747-A1 优先权日:2002-08-07 标 题 :Nanoliter-scale synthesis of arrayed biomaterials and screening thereof 发明人:ANDERSON DANIEL G; LEVENBERG SHULAMIT; LANGER ROBERT S 摘要:A method of screening cell-polymer interactions. The method includes depositing monomers as a plurality of discrete elements on a substrate, causing the deposited monomers to polymerize, thereby creating an array of discrete polymer elements on the substrate, incubating the substrate in a cell-containing culture medium, and characterizing a predetermined cell behavior on each polymer element.
专利号:WO-2005021522-A1 优先权日:2003-08-28 标 题:Synthesis of 1-‘4-(2-methoxyphenyl) piperazin-1-yl !-3-(2,6-dioxopiperidin-1-yl) propane 发明人:SALMAN MOHAMMAD; SHARMA SOMESH; YADAV GYAN CHAND 权利人:RANBAXY LAB LTD; SALMAN MOHAMMAD; SHARMA SOMESH; YADAV GYAN CHAND 摘要:The present invention relates to processes for the syntheses of 1-[4-(2-methoxyphenyl)piperazin-1-yl]-(2,6-dioxopiperidin-1-yl)propane and its pharmaceutically acceptable salts, preferably hydrochloride having uro-selective α1-adrenoceptor antagonistic activity. The compound holds promise for treating benign prostatic hyperplasia (BPH).
专利号:WO-2005021521-A1 优先权日:2003-08-28 标题:Preparation of 1-[4-(2-methoxy-phenyl)-piperazin-1-yl]-3-(2,6-dioxopiperidin-1-yl) propane hydrochloride 发明人:ANAND NITYA; SINHA NEELIMA; JAIN SANJAY; MEHTA ANITA 权利人:RANBAXY LAB LTD; ANAND NITYA; SINHA NEELIMA; JAIN SANJAY; MEHTA ANITA 摘要:The present invention relates to processes for the synthesis of 1-[4-(2Âmethoxyphenyl)piperazin-1-yl]-3-(2,6-dioxopiperidin-1-yl) propane hydrochloride having protracted uro-selective (α1-adrenoceptor antagonistic activity. The compound holds promise for treating benign prostatic hyperplasia (BPH).
专利号:WO-9919297-A9 优先权日:1997-10-15 标题 :Synthesis of azetidine derivatives 发明人:CHEN ZHENGMING; KOLB HARTMUTH C; RICHARDSON PAUL; HUANG ZHI-MIN 权利人:COELACANTH CHEMICAL CORP; CHEN ZHENGMING; KOLB HARTMUTH C; RICHARDSON PAUL; HUANG ZHI MIN 摘要:The present invention provides compound having formula (I) useful as building blocks for combinatorial libraries and methods of making such compounds. Also provided are compositions comprising the compounds.
专利号:US-6313297-B1 优先权日:1998-01-17 标题:Base-catalyzed synthesis of 1-aryl-4-(aryl ethyl)piperazines from aromatic olefins and 1-arylpiperazines 发明人:HERWIG JUERGEN; BELLER MATTHIAS; BREINDL CLAUDIA 权利人:AVENTIS RES & TECHNOLOGIES; GMBH & CO KG 摘要:A process for preparing a 1-aryl-4-(arylethyl)piperazine of the formula (I)by reacting a 1-arylpiperazine of the formula (II)with an aromatic olefin of the formula (III)in an inert solvent in the presence of at least one basic catalyst, where in the formulae (I) to (III)Ar and Ar' independently of one another are an aryl radical, selected from the group of the fused and unfused C6-C22-aromatics and the fused or unfused C5-C22-heteroaromatics which have at least one nitrogen, oxygen or sulfur atom in the ring; andR1 and R2 independently of one another are a hydrogen atom, a C1-C8-alkyl radical or an aryl radical Ar.
[参考文献]: Andrzej J Bojarski, Et Al. New Imide 5-Ht1A Receptor Ligands - Modification Of Terminal Fragment Geometry. Molecules. 2004 Feb 28;9(3):170-7. [参考文献]: Carl J Sennbro, Et Al. Determination Of Isocyanates In Air Using 1-(2-Methoxyphenyl)Piperazine-Impregnated Filters: Long-Term Sampling Performance And Field Comparison With Impingers With Dibutylamine. Ann Occup Hyg. 2004 Jul;48(5):415-24. [参考文献]: E Benfenati, Et Al. 1-(O-Methoxyphenyl)Piperazine Is A Metabolite Of Drugs Bearing A Methoxyphenylpiperazine Side-Chain. J Pharm Pharmacol. 1987 Apr;39(4):312-3. [参考文献]: Hartmut Henneken, Et Al. Validation Of A Diffusive Sampling Method For Airborne Low-Molecular Isocyanates Using 4-Nitro-7-Piperazinobenzo-2-Oxa-1,3-Diazole-Impregnated Filters And Liquid Chromatography-Tandem Mass Spectrometry. J Chromatogr A. 2006 Nov 17;1134(1-2):112-21. [参考文献]: Karen E Warburton, Et Al. Characterisation Of Derivatised Monomeric And Prepolymeric Isocyanates By Matrix-Assisted Laser Desorption/ionisation Time-Of-Flight Mass Spectrometry And Structural Elucidation By Tandem Mass Spectrometry. Eur J Mass Spectrom (Chichester). 2005;11(6):565-74.
合成参考文献
参考文献:10.1255/ejms.778 摘要:Warburton KE, Clench MR, Ford MJ, White J, Rimmer DA, Carolan VA. Characterisation of derivatised monomeric and prepolymeric isocyanates by matrix-assisted laser desorption/ionisation time-of-flight mass spectrometry and structural elucidation by tandem mass spectrometry. Eur J Mass Spectrom (Chichester). 2005;11(6):565–74. doi: 10.1255/ejms.778.