306934-84-9Relevant articles and documents
Nucleophilic Aromatic Substitution of Unactivated Aryl Fluorides with Primary Aliphatic Amines by Organic Photoredox Catalysis
Shi, Weimin,Zhang, Jingjie,Zhao, Fengqian,Wei, Wei,Liang, Fang,Zhang, Yin,Zhou, Shaolin
supporting information, p. 14823 - 14827 (2020/10/19)
In this work, a mild and transition-metal-free approach for the nucleophilic aromatic substitution (SNAr) of unactivated fluoroarenes with primary aliphatic amines to form aromatic amines is reported. This reaction is facilitated by the formati
Amines based on electron-rich fluoroaromatic hydrocarbons, and preparation method of amines
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Paragraph 0068-0071, (2019/10/15)
The invention provides amines based on electron-rich fluoroaromatic hydrocarbons, and a preparation method of the amines. The structure of the amines is as shown in a formula I. The invention also provides the preparation method of the amines based on the
Titanium-mediated amination of Grignard reagents using primary and secondary amines
Barker, Timothy J.,Jarvo, Elizabeth R.
, p. 8325 - 8328 (2011/10/31)
Make it, then break it: N-chlorosuccinimide (NCS) was employed as the oxidant in the synthesis of aniline derivatives using the title transformation (see scheme). Functionalization was well tolerated on both the amine and Grignard reagent. An androgen receptor agonist and several analogues were synthesized to demonstrate the utility of this method.
Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication
Skerlj, Renato,Bridger, Gary,Zhou, Yuanxi,Bourque, Elyse,McEachern, Ernest,Langille, Jonathan,Harwig, Curtis,Veale, Duane,Yang, Wen,Li, Tongshong,Zhu, Yongbao,Bey, Michael,Baird, Ian,Sartori, Michael,Metz, Markus,Mosi, Renee,Nelson, Kim,Bodart, Veronique,Wong, Rebecca,Fricker, Simon,Mac Farland, Ron,Huskens, Dana,Schols, Dominique
scheme or table, p. 6950 - 6954 (2012/01/13)
A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of α-glycoprotein were evaluated in rat and dog pharmacokinetics.
AMINOPIPERIDINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
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Page/Page column 21, (2010/11/28)
The present invention relates to compounds of formula (I) as defined herein that are melanocortin receptor agonists, to the preparation thereof and to the therapeutic use thereof in the treatment and in the prevention of obesity, diabetes and sexual dysfunctions that can affect both sexes, in the treatment of cardiovascular diseases, and also in anti-inflammatory uses or in the treatment of alcohol dependency.
ERYTHROPOIETIN PRODUCTION ACCELERATOR
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Page/Page column 82, (2008/06/13)
The present invention relates to a preventive or therapeutic agent for pathological conditions caused by reduced production of erythropoietin, or for anemia, or for chronic anemia, renal anemia, aplastic anemia, or pure red cell aplasia, the agent comprising, as an active ingredient, a cyclic amine compound represented by the following formula (1): wherein, ???R1, R2 and R3 each independently represent a hydrogen atom, a halogen atom, or hydroxy, alkyl, halogen-substituted alkyl, alkoxy, alkylthio, carboxyl, alkoxycarbonyl or alkanoyl group; ???W1 and W2 each independently represent N or CH; ???X represents O, NR4, CONR4 or NR4CO; ???R4 each represents a hydrogen atom, or an alkyl, alkenyl, alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aralkyl, or substituted or unsubstituted heteroaralkyl group; and ???l, m and n each represents a number of 0 or 1, or a salt thereof or a solvate thereof.
Cyclic amine compounds and pharmaceutical composition containing the same
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, (2008/06/13)
A cyclic amine compound by the following general formula (1): wherein, R1, R2and R3each independently represent a hydrogen atom or an alkoxy group W1and W2each independently represent N or CH; X represents O, NR4, CONR4or NR4CO; R4represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.
Multistep solution-phase parallel synthesis of spiperone analogues
Hansen, Henrik C.,Olsson, Roger,Croston, Glenn,Andersson, Carl-Magnus
, p. 2435 - 2439 (2007/10/03)
A flexible, multistep parallel synthesis of spiperone analogues is described. A library of 4-substituted piperidines, assembled utilizing reductive amination and acylation protocols, was alkylated either homogeneously or heterogeneously, exploiting a product release only concept, to afford an oxa-series of spiperone analogues. Screening of the products at 5-HT2 and D2 receptors revealed 5-HT(2A) antagonists with improved selectivity compared to spiperone and AMI-193. (C) 2000 Published by Elsevier Science Ltd.