CAS: 637-32-1; N-(4-Chlorophenyl)-N′-(1-Methylethyl)Imidodicarbonimidic Diamide Monohydrochloride

该化合物是一种主要用作抗疟剂的合成重聚物化合物,其功能是抑制寄生虫中的二氢氟化硫还原酶酶,破坏叶酸新陈代谢,防止DNA合成;盐酸盐形式可提高溶性,使其适合口服,其关键优势包括:对易感染疟疾菌株的成熟功效简介,以及临床使用中有利的安全保障.氯甲酸盐因其长期行动和成本效益,常常被用于预防疗法中.该化合物也是制药研究中进一步衍生的前体.建议在干燥条件下适当储存,以保持稳定.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

合成工艺路线路线简述

    📜P-Chlorophenyl Cyanoguanidine,异丙胺,氨,Disodium;2-[2-[bis(Carboxymethyl)Amino]Ethyl-(Carboxylatomethyl)Amino]Acetate置于copper Sulfate Pentahydrate P-Chlorophenyl Cyanoguanidine,乙二胺四乙酸,水体系中,用 水 作为反应溶剂,化学反应 10.5H,反应生成 吉非罗齐杂质a
    参考文献:Process Of Preparation Of Proguanil
    标题:Process Of Preparation Of Proguanil
    摘要:本文揭示了1-(4-氯苯基)-5-异丙基双胍盐酸盐(盐酸普罗硅嗪),公式-I,一种抗疟疾药物的制备过程.

    海关参考信息

    专利信息


    专利号:US-2024287041-A1
    优先权日:2021-05-20
    标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
    发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
    权利人:KARYOPHARM THERAPEUTICS INC
    摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

    专利号:US-9765042-B2
    优先权日:2013-10-07
    标题 :Methods of chemical synthesis of diaminophenothiazinium compounds including methylthioninium chloride (MTC)
    发明人:SINCLAIR JAMES PETER; NICOLL SARAH LOUISE; STOREY JOHN MERVYN DAVID
    权利人:WISTA LAB LTD
    摘要:Methods of synthesizing and purifying certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compoundsâ€?) including Methythioninium Chloride (MTC) (also known as Methylene Blue) are provided.

    专利号:US-2006287257-A1
    优先权日:2005-06-20
    标 题 :Pharmaceutical compositions to treat diseases caused by mycobacterium
    发明人:STOCKEL RICHARD F
    权利人:STOCKEL RICHARD F
    摘要:The invention teaches the synthesis of pharmaceutical composition and methods of synthesis to treat people and animals infected with a pathogenic mycobacterium. In particular the compositions of this invention are suitable for the treatment of tuberculosis, malaria, and other infections diseases caused by mycobacterium.

    专利号:US-7790881-B2
    优先权日:2004-09-23
    标 题:Methods of chemical synthesis and purification of diaminophenothiazinium compounds including methylthioninium chloride (MTC)
    发明人:STOREY JOHN MERVYN DAVID; SINCLAIR JAMES PETER; MARSHALL COLIN; TAN HAN WAN
    权利人:WISTA LAB LTD
    摘要:This invention pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesizing and purifying certain 3,7 diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compoundsâ€?) including Methylthioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the method comprises the steps of, in order: nitrosylation (NOS); nitrosyl reduction (NR); thiosulfonic acid formation (TSAF); oxidative coupling (OC); Cr(VI) reduction (CR); isolation and purification of zwitterionic intermediate (IAPOZI); ring closure (RC); chloride salt formation (CSF); one of: sulphide treatment (ST); dimethyldithiocarbamate treatment (DT); carbonate treatment (CT); ethylenediaminetetraacetic acid treatment (EDTAT); organic extraction (OE); and recrystallisation (RX). The present invention also pertains to the resulting (high purity) compounds, compositions comprising them (e.g., tablets, capsules), and their use in methods of inactivating pathogens, and methods of medical treatment and diagnosis, etc., for example, for tauopathies, Alzheimer's disease (AD), skin cancer, melanoma, viral diseases, bacterial diseases, or protozoal diseases. Wherein: each of R 1 and R 9 is independently selected from: —H; C 1-4 alkenyl; and halogenated C 1-4 alkyl; each of R 3NA and R 3NB is independently selected from: C 1-4 alkyl; C 2-4 alkenyl; and halogenated C 4-1 alkyl; each of R 7NA and R 7NB is independently selected from: C 1-4 alkyl; C 2-4 alkenyl; and halogenated C 1-4 alkyl; and X is one or more anionic counter ions to achieve electrical neutrality.

    专利号:AU-2022276509-A1
    优先权日:2021-05-20
    标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

    专利号:US-9994558-B2
    优先权日:2013-09-20
    标题 :Multicyclic compounds and methods of using same
    发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON
    权利人:KARYOPHARM THERAPEUTICS INC
    摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Kuemmerle A, Gossen D, Marx MW, Lorch U, Szramowska M, Kumar A, Singh D, Singh S, Ramachandruni H, Thankachen B, Kore S, Gaaloul ME, Borghini-Fuhrer I, Chalon S. A randomized, open-label two-period crossover pilot study to evaluate the relative bioavailability in the fed state of atovaquone-proguanil (Atoguanil™) versus atovaquone-proguanil hydrochloride (Malarone®) in healthy adult participants. Naunyn Schmiedebergs Arch Pharmacol. 2024 Jun 25. doi: 10.1007/s00210-024-03245-x. Epub ahead of print.
    225:106179. doi: 10.1016/j.actatropica.2021.106179. Epub 2021 Oct 8. 45(6):376-383. doi: 10.1080/01913123.2021.1984349. Epub 2021 Oct 1. 12(1):10.24926/iip.v12i1.3555. doi: 10.24926/iip.v12i1.3555.
    5: Lee SH, Kwak D, Kim KT. The first clinical cases of Haemoproteus infection in a snowy owl (Bubo scandiacus) and a goshawk (Accipiter gentilis) at a zoo in the Republic of Korea. J Vet Med Sci. 2018 Aug 10;80(8):1255-1258. doi: 10.1292/jvms.18-0072. Epub 2018 Jun 22.

    合成参考文献


    摘要:Journal of Pharmacology and Experimental Therapeutics., 91(157), 1947
    参考文献:10.1007/s00228-002-0426-9
    摘要:Thapar MM, Ashton M, Lindegårdh N, Bergqvist Y, Nivelius S, Johansson I, Björkman A. Time-dependent pharmacokinetics and drug metabolism of atovaquone plus proguanil (Malarone) when taken as chemoprophylaxis. European Journal of Clinical Pharmacology. 2002 Feb 28;58(1):19–27. doi: 10.1007/s00228-002-0426-9.
    参考文献:10.1186/1475-2875-10-141
    摘要:Tommasi C, Bellagamba R, Tempestilli M, D'Avolio A, Gallo AL, Ivanovic J, Nicastri E, Pucillo LP, Narciso P. Marked increase in etravirine and saquinavir plasma concentrations during atovaquone/proguanil prophylaxis. Malaria Journal. 2011 May 21;10(1):141. doi: 10.1186/1475-2875-10-141.
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