CAS: 4975-73-9; N,N'-Dicyclohexylmorpholine-4-Carboximidamide

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CAS号110-91-8 吗啉 | CAS号538-75-0 N,N'-二环己基碳酰亚胺 | CAS号36903-85-2 (cyclohexylamin... | CAS号117688-40-1 1,1'-hexamethyl...

合成工艺路线路线简述

    (Cyclohexylamino)Morpholin-4-Ylmethane-1-Thione置于cocl2体系中,用 四氢呋喃,氯仿 作为反应溶剂,化学反应 22.0H,反应生成 N,N'-二环己基-4-吗啉脒
    参考文献:N,N'-二环己基-4-吗啉羧box的烷基和芳基胍类似物的合成及其利尿活性.
    标题:N,N'-二环己基-4-吗啉羧box的烷基和芳基胍类似物的合成及其利尿活性.
    摘要:随机筛选确定n,N'-二环己基-4-吗啉羧box(u-18177,1)为大鼠口服有效的非利尿剂利尿剂.在狗中口服1和其1-金刚烷基类似物(u-37883A,4)的利尿特性时,它们的功效不如标准利尿剂,但在>或= 100 Mumol / Kg时显示了速尿类似的利尿作用.但是,急性1在61和90 Mumol / Kg Iv静脉注射可导致犬致命的心脏毒性.1的许多类似物在质上表现出相似的利尿特性,但没有一个足以保证发育.化合物1还逆转了米诺地尔在犬中的血管舒张作用,这导致了血管相互作用的研究表明,类似物4可能会阻断atp敏感的k通道.这种钾通道阻滞机制可能有助于该系列的利尿活性.
    DOI:10.1021/jm00048A005

    海关参考信息

    专利信息


    专利号:WO-9222662-A1
    优先权日:1991-06-10
    标 题:Methods for the synthesis of monofucosylated oligosaccharides terminating in di-n-acetyllactosaminyl structures
    发明人:VENOT ANDRE P; KASHEM MOHAMMED A; SMITH RICHARD H
    权利人:ALBERTA RES COUNCIL
    摘要:Disclosed are methods for the preparation of monofucosylated and sialylated derivatives of the compound $g(b)Gal(1-4)$g(b)GlcNAc(1-3)$g(b)Gal(1-4)$g(b)GlcNAc-R. In particular, the methods of this invention provide for a multi-step synthesis wherein selective monofucosylation is accomplished on the 3-hydroxy group on only one of the GlcNAc units found in the $g(b)Gal(1-4)$g(b)GlcNAc(1-3)$g(b)Gal(1-4)$g(b)GlcNAc-R compound. In this step, monofucosylation is achieved by use of the $g(a)(1-3)fucosyltransferase.

    专利号:US-9303051-B2
    优先权日:2010-08-31
    标 题 :Phosphonate ester derivatives and methods of synthesis thereof
    发明人:WARE ROY W; ALMOND MERRICK R; LAMPERT BERNHARD M
    权利人:CHIMERIX INC; CHIMERIX INC
    摘要:The disclosure describes methods of synthesis of phosphonate ester derivatives. Preferred methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of phosphonate ester derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of phosphonate ester derivatives.

    专利号:US-5770407-A
    优先权日:1996-12-10
    标题:Process for preparing nucleotide inhibitors of glycosyltransferases
    发明人:WONG CHI-HUEY; HAYASHI TAKASHI
    权利人:SCRIPPS RESEARCH INST
    摘要:Nucleotide linked 2-deoxy-2-fluoroglycosides are employed as potent competitive inhibitors of glycosyltransferases. More particularly, uridine-5'-diphospho-2-deoxy-2-fluoro-galactose (UDP-2F-Gal), guanidine-5'-diphospho-2-deoxy-2-fluoro-L-fucose (GDP-2F-Fuc), uridine-51-diphospho-2-deoxy-2-fluoro-D-glucose (UDP-2F-Glu), guanosine-5'-diphospho-2-deoxy-2-fluoro-D-mannose (GDP-2F-Man), cytosine-5'-monophospho-2-deoxy-2-fluoro-D-sialic acid, and cytosine-5'-monophospho-2-deoxy-2-KDO may be employed as inhibitors of β-1,4-galactosyltransferase, α-1,3-fucosyltransferase, glucosyltransferases, N-acetylglucosaminyltransferases, (α-mannosyltransferases, α-sialyltransferases, and KDO-transferases, respectively. Synthesis of nucleotide-linked-2-deoxy-2-fluoroglycosides is achieved using either chemoenzymatic or chemical methodologies.

    专利号:US-5550155-A
    优先权日:1991-06-10
    标 题:Methods for the synthesis of monofucosylated oligosaccharides terminating in di-N-acetyllactosaminyl structures
    发明人:KASHEM MOHAMMED A; VENOT ANDRE P; SMITH RICHARD
    权利人:ALBERTA RES COUNCIL
    摘要:Monofucosylated and monosialyated derivatives of the compound βGal(1-4)βGlcNAc(1-3)βGal(1-4)βGlcNAc-OR, where R is hydrogen, a saccharide, an oligosaccharide or an aglycon moiety have been found to be useful in modulating a cell-mediated immune inflammatory response in mammals.

    专利号:US-5882901-A
    优先权日:1991-06-10
    标 题:Modified sialyl Lewisa compounds
    发明人:VENOT ANDRE P; NIKRAD PANDURANG V; KASHEM MOHAMMED A
    权利人:ALBERTA RES COUNCIL
    摘要:The present invention is drawn to methods for the synthesis of Lewis a derivatives modified at the C-2 and/or C-6 position of GlcNAc employing chemo-enzymatic synthesis. The derivatives find use in the treatment and prevention of diseases.

    专利号:US-5939290-A
    优先权日:1991-06-10
    标题 :Modified sialyl Lewisx compounds
    发明人:VENOT ANDRE P; NIKRAD PANDURANG V; KASHEM MOHAMMED A
    权利人:ALBERTA RES COUNCIL
    摘要:The present invention is drawn to methods for the synthesis of sialyl Lewis x derivatives modified at the C-2 and/or C-6 position of GlcNAc employing chemoenzymatic synthesis. The derivatives find use in the treatment and prevention of diseases.
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    主要参考文献

    [参考文献]: Earl R Kern, Et Al. Enhanced Inhibition Of Orthopoxvirus Replication In Vitro By Alkoxyalkyl Esters Of Cidofovir And Cyclic Cidofovir. Antimicrob Agents Chemother. 2002 Apr;46(4):991-5.
    [参考文献]: S C Perricone, Et Al. Synthesis And Diuretic Activity Of Alkyl- And Arylguanidine Analogs Of N,N'-Dicyclohexyl-4-Morpholinecarboxamidine In Rats And Dogs. J Med Chem. 1994 Oct 28;37(22):3693-700.

    合成参考文献


    摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#07096
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