CAS: 65472-88-0; (E)-N-Methyl-N-(Naphthalen-1-Ylmethyl)-3-Phenylprop-2-En-1-Amine

该化合物是合成的甲胺衍生物,具有强效抗风素特性,主要用于治疗皮肤纤维素和直肠丝虫,其行动机制包括抑制乙氧基乙酰,乙醇生物合成物中的一种关键酶,导致真菌细胞膜干扰. (E)-Naftifine展示了针对三氯酚,乙酰甲胺酮和康迪达物种的广泛活动,其效力高于老的阿索抗风素.该化合物展示了真菌和抗肺炎效应,加强了其治疗特征.其可喜的致癌基因可以进行时事管理,最大限度地减少系统接触. (E)-Naftifine因其迅速开始行动并降低抗药性,因此被评价为抗风素疗法的可靠选择.

结构式图片

上下游产品

CAS号50-00-0 甲醛 | CAS号92610-10-1 N-(naphthalen-1... | CAS号16519-25-8 Benzene,(3-phen... | CAS号14489-75-9 N-甲基-1-萘甲胺 | CAS号4407-36-7 3-苯基-2-丙烯-1-醇; ... | CAS号4393-06-0 1-苯基-2-丙烯-1-醇 | CAS号1334031-95-6 (E)-methyl cinn... | CAS号118-31-0 1-萘甲胺 | CAS号4780-79-4 1-萘甲醇 | CAS号60960-88-5 N-甲基肉桂基胺

合成工艺路线路线简述

    N-Cinnamyl-N-Methyl-1-Naphthylamide置于lithium Aluminium Tetrahydride体系中,用 乙醚 作为反应溶剂,以89%的收率获得产物萘替芬
    参考文献:一种胺类化合物及其制备方法与应用
    标题:一种胺类化合物及其制备方法与应用
    摘要:本发明公开了一种含有烯丙基或苄基的胺类化合物及其制备方法与应用.本发明通过将原料1,胺,催化剂,添加剂依次加入到反应溶剂中,在空气氛围和50~120oc条件下搅拌反应12~24H,得到反应液;其中,所述原料1为烯丙醇或苄醇;所述原料1,胺,催化剂,添加剂和反应溶剂的摩尔体积比为(0.2~8)Mmol:(0.4~12)Mmol:(0.01~0.4)Mmol:(0.01~0.4)Mmol:(2~40)Ml;除去所述反应液的反应溶剂,再通过薄层层析法/柱层析法纯化,展开剂体系为石油醚/乙酸乙酯,得到含有烯丙基或苄基的胺类化合物.该胺类化合物可应用在生物和药物活性分子的骨架的制备中.本发明制备方法适用的底物范围广泛,操作方便,绿色环保.

    海关参考信息

    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:US-2024336559-A1
    优先权日:2021-10-06
    标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids
    发明人:OJIMA IWAO; HARANAHALLI KRUPANANDAN; DEL POETA MAURIZIO; GARG ASHNA
    权利人:UNIV NEW YORK STATE RES FOUND
    摘要:The present invention provides a compound having the structure: n n n n n n n n n n n n wherein n R 3 , R 4 , R 5 , R 6 , and R 7 are each independently, H, halogen, CN, —CF 3 , —OCF 3 , —NO 2 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, —OH, —OAc, —OR 13 , —COR 13 , —CH 2 OR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ; n R 9 , R 10 , R 11 , and R 12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, —OAc, —COR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ;n wherein each occurrence of R 13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 14 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 15 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, n n wherein when R 14 is methyl, R 15 is not methyl; n wherein at least one of R 9 , R 10 , R 11 , and R 12 is not H; n wherein at least one of R 3 , R 4 , R 5 , R 6 , and R 7 is not H.

    专利号:US-8106031-B2
    优先权日:2006-05-02
    标题:Hydrolytically-resistant boron-containing therapeutics and methods of use
    发明人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A
    权利人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A; ANACOR PHARMACEUTICALS INC
    摘要:Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.

    专利号:US-7935704-B2
    优先权日:2003-08-01
    标 题 :Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
    发明人:PALLADINO MICHAEL A; LLOYD GEORGE KENNETH; HAYASHI YOSHIO; NICHOLSON BENJAMIN
    权利人:NEREUS PHARMACEUTICALS INC
    摘要:Compounds represented by the following structure (I) are disclosed: n nas are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ′, R 1 ″, R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.

    专利号:US-7956058-B2
    优先权日:2002-08-02
    标 题:Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
    发明人:HAYASHI YOSHIO; PALLADINO JR MICHAEL A; GRODBERG JENNIFER
    权利人:NEREUS PHARMACEUTICALS INC
    摘要:Compounds represented by the following structure (I) are disclosed: n nas are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ′, R 1 ′, R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating cancer and fungal infection are also disclosed.

    专利号:US-9382288-B2
    优先权日:2010-10-06
    标题 :Derivatives of steroid benzylamines, having an antiparasitic antibacterial, antimycotic and/or antiviral action
    发明人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO
    权利人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO; UNIV GIESSEN JUSTUS LIEBIG
    摘要:The present invention relates to compounds derived from steroids of the general formula (I) n nwherein L represents a linker and R # represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).
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    合成参考文献


    摘要:Ewing, T. A.; Fraaije, M. W.; van Berkel, W. J. H., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 3, 177.
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    参考文献:10.1016/j.ejmech.2020.112645
    摘要:Sun B, Dong Y, An Y, Liu M, Han J, Zhao L, Liu X. Design, synthesis and bioactivity evaluation of novel arylalkene-amide derivatives as dual-target antifungal inhibitors. European Journal of Medicinal Chemistry. 2020 Nov;205():112645. doi: 10.1016/j.ejmech.2020.112645.
    参考文献:10.1007/bf00436392
    摘要:Butty P, Mallié M, Bastide JM. Antifungal activity of allylamines on Epidermophyton floccosum: scanning electron microscopy study. Mycopathologia. 1992 Dec;120(3):147–53. doi: 10.1007/bf00436392.
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