CAS: 50541-93-0; 4-Amino-1-Benzylpiperidine

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CAS号949-69-9 1-苄基-4-哌啶酮肟 | CAS号4783-65-7 1-苄基-2-哌啶酮 | CAS号64-17-5 乙醇 | CAS号62992-68-1 1-苄基哌啶-4-羧酰胺 | CAS号73889-19-7 1-苄基-4-(B°C-氨基)哌啶 | CAS号3612-20-2 N-苄基-4-哌啶酮 | CAS号100-39-0 溴化苄 | CAS号50534-33-3 2-[1-(Phenylmet... | CAS号74045-91-3 1-苄基哌啶-4-甲酰肼 | CAS号100-44-7 氯化苄 | CAS号33953-37-6 4-苯甲酰氨基哌啶 水合物 | CAS号50534-23-1 4-乙酰氨基-1-苄基哌啶 | CAS号91596-61-1 1-哌啶-4-基-吡咯烷-2-酮 | CAS号209223-86-9 N-(1-benzylpipe... | CAS号208184-69-4 N-(1-benzylpipe... | CAS号185058-54-2 N-(1-Benzylpipe... | CAS号208184-80-9 N-(1-benzylpipe... | CAS号303763-39-5 4-(TERT-BUTOXYC... | CAS号303763-37-3 1-[(6-溴吡啶- 2-基)... | CAS号87120-72-7 1-B°C-4-氨基哌啶

N-苄基哌啶酮置于lithium Aluminium Tetrahydride,盐酸羟胺,Potassium Carbonate体系中,用 四氢呋喃,乙醇 作为反应溶剂,化学反应 12.0H,反应生成 4-氨基-1-苄基哌啶
参考文献:作为潜在乙酰胆碱酯酶抑制剂的新型 3-羟基吡啶-4-酮衍生物的设计,合成,分子对接和分子动力学模拟研究
标题:作为潜在乙酰胆碱酯酶抑制剂的新型 3-羟基吡啶-4-酮衍生物的设计,合成,分子对接和分子动力学模拟研究
摘要:研究人员专注于抑制乙酰胆碱酯酶来治疗阿尔茨海默病.在本研究中,使用羟基吡啶-4-一加上苄基哌啶支架合成了一些新型ache抑制剂,并使用ellman方法对其进行了评估.因此,与多奈哌齐相比,((1-(4-甲氧基苯乙基)哌啶-4-基)氨基)甲基)-5-羟基-1-甲基吡啶-4(1H)-酮(Vii D)显示出较弱但有希望的ache抑制作用. Ic 50 =143.090Nm).发现vii D的平均 Rmsd 值为2.25,表明活性位点残基的结构变化较小.viid的苯基-乙基-N-哌啶部分的苯基与trp285和tyr340形成疏水相互作用.哌啶环的氮原子与phe294之间存在π-阳离子相互作用.在连接子的 2 型胺和 Trp85 之间发现了另一种 π 阳离子相互作用.哌啶环通过疏水相互作用与 Tyr336,Tyr123 和 Phe337 相互作用.事实上,Vii D预计会通过胃肠道被吸收,尽管它可能被
DOI:10.1002/cbdv.202300325

专利信息

专利号:US-5877278-A
优先权日:1992-09-24
标题:Synthesis of N-substituted oligomers
发明人：ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA
权利人:CHIRON CORP
摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.

专利号:US-9765027-B2
优先权日:2014-08-22
标题 :Substituted 1-arylethyl-4-acylaminopiperidine derivatives as opioid/alpha-adrenoreceptor modulators and method of their preparation
发明人：VARDANYAN RUBEN S; HRUBY VICTOR J
权利人:THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZAONA; UNIV ARIZONA
摘要:The invention provides compounds that bind with high affinities to the μ-, δ- and κ-opioid receptors and α 2 -adrenoreceptor. In addition to providing these compounds with novel pharmacological binding properties, the invention also describes detailed novel methods for the preparation of representative compounds and a scheme for the synthesis of related compounds that bind to the opioid receptors and/or α 2 -adrenoreceptor.

专利号:WO-0110798-A1
优先权日:1999-08-04
标题 :Solid phase synthesis of oxa- and thiazoles
发明人：BUNIN BARRY A; TUSHUP STEVEN P
权利人:CHEMRX ADVANCED TECHNOLOGIES I; BUNIN BARRY A; TUSHUP STEVEN P
摘要:Thia- and oxazole-4-carboxylic acid derivatives are prepared by solid phase synthesis, using intermediates of formula (α) where SS is a solid support and n is 0 or 1.

专利号:US-9890126-B2
优先权日:2012-04-24
标 题:Synthesis of novel inhibitors of isoprenoid biosynthesis (ISPF)
发明人：HAGEN TIMOTHY J; ZHANG ZHENG; LAZOWSKI ZACHARY; CLARE MICHAEL; BEGLEY DARREN W
权利人:UNIV NORTHERN ILLINOIS BOARD OF TRUSTEES; BERYLLIUM DISCOVERY CORP
摘要:Antibacterial and antimalarial IspF inhibitor compounds and compositions are described. Methods include administering described compounds and compositions to treat bacterial or parasitic infections and to inhibit parasite or bacterial growth.

专利号:US-6420556-B1
优先权日:1998-12-17
标 题 :Acyl isothiocyanate resins and their use in solid-supported synthesis of guanidines
发明人：WILSON LAWRENCE JOSEPH
权利人:PROCTER & GAMBLE
摘要:The subject invention involves novel acyl isothiocyanate resins of formula (I) and processes for making them: (a) starting with a phenyl carboxy resin, treating the resin with any reagent that converts the carboxy to an acyl halide, followed by treatment with tetranikylammonium thiocyanate or an alkali metal salt thereof, to provide the acyl isothiocyanate resin. The subject invention also involves processes for making guanidine compounds and related cyclized compounds using an acyl isothiocyanate resin, comprising the following steps: (b) reacting the acyl isothiocyanate resin with a primary amine; (c) reacting the product from Step (b) with a sulfur activating agent and ammonia or a primary or secondary amine; (d) treating the product from Step (c) with a strong base or medium strength acid to cleave product from the resin, providing the guanidine compound or/and the related cyclized compound.

专利号:US-2003092064-A1
优先权日:2001-04-05
标题 :System for the synthesis of spatially separated libraries of compounds and methods for the use thereof
发明人：READER JOHN C
权利人:MILLENNIUM PHARM INC
摘要:Featured is an apparatus useful for preparing combinatorial libraries of compounds in a parallel fashion so that the individual compounds of the library are spatially separate and the position of each compound of the library in the apparatus is known. Moreover, the apparatus is useful for the preparation of combinatorial libraries of compounds where the library is constructed from three or more building blocks, e.g., three, four, five, six or seven building blocks, resulting in a three, four, five, six or seven dimensional combinatorial library. Also featured are related methods for the preparation of three, four, five, six or seven dimensional combinatorial libraries of compounds using the apparatus of the present invention.