CAS: 90-89-1; N,N-Diethylcarbamazine

该化合物是一种专门的有机化合物,在4级以一组甲基人取代一组人,在1级以二乙基碳本胺取代一组人,这种结构具有独特的物理化学特性,使其作为制药和农用化学合成的中间体具有宝贵价值.该化合物的界定明确的立体化学和功能组兼容性增强了其在生物活性分子开发中的效用.在标准条件下的稳定性和普通有机溶剂的溶解性促进了合成工作流程的直截了当处理.三级和氨基功能的存在都为进一步衍生提供了多功能,支持了医药化学和材料科学的应用.

结构式图片

欧盟法规

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上下游产品

1-methyl-piperazine O-phenyl N,N-diethylcarbamate N,N-diethylcarbamyl chloride 4-methyl-piperazine-1-carbonyl chloride4-diethylcarbamoyl-1-methyl-1-tetradecyl-piperazinium; bromide

合成工艺路线路线简述

  • 109-01-3 + 88-10-8 = 90-89-1 [标题:Reaction Conditions
    标题:Experimental Chemotherapy Of Filariasis. V. The Preparation Of Derivatives Of Piperazine
    作者:Kushner,S.; Brancone,L. M.; Hewitt,R. I.; Mcewen,W. L.; Subbarow,Y.; Et Al
    参考文献:Journal Of Organic Chemistry 日期:1948 卷标:13 页码:144-53]

    119-54-0 = 90-89-1 [标题:Reaction Conditions
    标题:1-Diethylcarbamoyl-4-Methylpiperazine
    参考文献:Ussr
N,N-二乙基氯甲酰胺置于甲酸,乙醇体系中,化学反应生成 乙胺嗪
参考文献:实验性丝虫病化学疗法;制备哌嗪的衍生物.
标题:实验性丝虫病化学疗法;制备哌嗪的衍生物.
摘要:
DOI:10.1021/jo01159A019

海关参考信息

专利信息


专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人:MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

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).

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:KR-101513003-B1
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy compositions and applications

专利号:US-9907753-B2
优先权日:2010-03-19
标 题 :Lipid vesicle compositions and methods of use
发明人:IRVINE DARRELL J; MOON JAEHYUN
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The invention provides delivery systems comprised of stabilized multilamellar vesicles, as well as compositions, methods of synthesis, and methods of use thereof. The stabilized multilamellar vesicles may comprise prophylactic, therapeutic and/or diagnostic agents.

专利号:CN-117946033-A
优先权日:2023-12-18
标题 :Preparation method for photo-promoted synthesis of urea compound
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主要参考文献


1: Abdel-Latif M, Sakran T, El-Shahawi G, El-Fayoumi H, El-Mallah AM. Effect of diethylcarbamazine citrate and Setaria equina excretory-secretory material on rat hepatocellular carcinoma. Arch Immunol Ther Exp (Warsz). 2014 Dec;62(6):511-20. doi: 10.1007/s00005-014-0292-z. Epub 2014 May 31. doi: 10.1517/17425247.2014.915310. Epub 2014 May 21. doi: 10.1186/s13071-015-1122-9.
4: Schmidt MS, King CL, Thomsen EK, Siba PM, Sanuku N, Fleckenstein L. Liquid chromatography-mass spectrometry analysis of diethylcarbamazine in human plasma for clinical pharmacokinetic studies. J Pharm Biomed Anal. 2014 Sep;98:307-10. doi: 10.1016/j.jpba.2014.05.016. Epub 2014 May 22. doi: 10.1016/j.xphs.2016.06.003. Epub 2016 Jul 7. doi: 10.1093/cid/civ882. Epub 2015 Oct 20. doi: 10.1016/j.ejphar.2012.05.044. Epub 2012 Jun 7. doi: 10.1016/j.actatropica.2010.09.009. Epub 2010 Oct 8. doi: 10.1007/s00436-013-3696-5. Epub 2013 Dec 24. doi: 10.1016/j.parint.2011.06.019. Epub 2011 Jun 24. doi: 10.1007/s10900-014-9891-1.

合成参考文献


参考文献:10.1186/1756-3305-4-134
摘要:Ashton RA, Kyabayinze DJ, Opio T, Auma A, Edwards T, Matwale G, Onapa A, Brooker S, Kolaczinski JH. The impact of mass drug administration and long-lasting insecticidal net distribution on Wuchereria bancrofti infection in humans and mosquitoes: an observational study in northern Uganda. Parasites & Vectors. 2011 Jul 15;4(1):134. doi: 10.1186/1756-3305-4-134.
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