CAS: 500-92-5; 1-Isopropyl-5-(4-Chlorophenyl)Biguanide

该化合物是一种主要用于预防和治疗疟疾的抗疟药物,是一种属于重原类药物的合成化合物.Proguanil作为一种药物,它作为一种药物,在身体中代谢成其活性形式环状环状,抑制了疟疾寄生虫中的二氢氟酸还原酶酶,干扰了泡沫合成,并最终阻碍了其生长和生殖.该物质一般是口服的,并已知其毒性相对较低,在人类中具有良好的耐药性.Progual经常与其他抗疟剂(如阿托瓦酮)结合使用,以提高其功效并降低抗药性风险.就物理特性而言,Proguanil是一种白白对在水中可溶解并具有中分子重量的脱色晶粉.其致药性包括快速吸收和半衰期支持一次服用疟疾的半衰期,使其成为疟疾预防的方便选择.

结构式图片

上下游产品

CAS号1482-62-8 1-(4-氯苯基)-3-氰基胍 | CAS号75-31-0 异丙胺 | CAS号44830-55-9 氯胍杂质A | CAS号20265-96-7 对氯苯胺盐酸盐 | CAS号15572-56-2 异丙胺盐酸盐 | CAS号79491-01-3 3-[(4-chlorophe... | CAS号857592-68-8 S-ethyl-N-(4-ch... | CAS号857592-70-2 S-ethyl-N-(4-ch... | CAS号13463-94-0 (4-chlorophenyl...

合成工艺路线路线简述

    📜1-异丙基-5-苯基双胍置于氯体系中,化学反应生成 氯胍
    参考文献:Crowther Et Al.,Journal Of The Chemical Society,1951,P. 1774,1778
    标题:Crowther Et Al.,Journal Of The Chemical Society,1951,P. 1774,1778

    海关参考信息

    专利信息


    专利号:US-8680276-B2
    优先权日:2009-03-06
    标题 :Synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine
    发明人:MOTTERLE RICCARDO; ARVOTTI GIANCARLO; BERGANTINO ELISABETTA; CASTELLIN ANDREA; FOGAL STEFANO; GALVAGNI MARCO
    权利人:MOTTERLE RICCARDO; ARVOTTI GIANCARLO; BERGANTINO ELISABETTA; CASTELLIN ANDREA; FOGAL STEFANO; GALVAGNI MARCO
    摘要:The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.

    专利号:US-2012100555-A1
    优先权日:2009-06-29
    标题 :Synthesis And Use Of Fluorophore-Tagged Antimalarials
    发明人:LEAR MARTIN JAMES; TAN KEVIN SHYONG WEI
    权利人:LEAR MARTIN JAMES; TAN KEVIN SHYONG WEI
    摘要:This invention includes a fluorophore-tagged antimalarial represented by the following structural formula (1) or a salt thereof. This invention relates to the synthesis of fluorophore-tagged antimalarials and describes the synthesis of a fluorophore-tagged antimalarial. These fluorophore-tagged antimalarials can be used to image live cells to determine the location of the antimalarial in the cell, identify drug resistance and growth related pathways in Plasmodium isolates, identify new drug targets and chemo-sensitizers to reverse drug resistance.

    专利号:US-9409879-B2
    优先权日:2011-03-29
    标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents
    发明人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA
    权利人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA; CENTRE NAT RECH SCIENT
    摘要:Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents.

    专利号:US-7947701-B2
    优先权日:2003-11-14
    标题:Dual molecules containing peroxy derivative, the synthesis and therapeutic applications thereof
    发明人:CAZELLES JEROME; COSLEDAN FREDERIC; MEUNIER BERNARD; PELLET ALAIN
    权利人:SANOFI AVENTIS
    摘要:The invention relates to dual molecule compounds containing a peroxide derivative, to processes for the synthesis of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment and prevention of malaria comprising administering such compounds and such pharmaceutical compositions.

    专利号:US-4891430-A
    优先权日:1984-12-04
    标 题:Process for synthesizing active esters of carboxylic acids, new alpha-halogenated carbonates which are useful for this synthesis and the method of producing them
    发明人:BARCELO GERARD; CASTRO BERTRAND; JAOUADI MAHMOUD; MARTINEZ JEAN; SENET JEAN-PIERRE; SENNYEY GERARD
    权利人:INT DES POUDRES ET EXPLOSIFS S
    摘要:The invention relates to a new process for preparing active esters or carboyxlic acids, which consists in reacting a carboxylic acid, in the presence of an agent for binding hydrohalic acid, with a carbonate of formula: ##STR1## in which R 1 denotes either a radical of formula ##STR2## in which R 3 and R 4 , which may be identical or different, are not hydrogen atoms and denote organic radicals which may be substituted or unsubstituted and saturated or unsaturated, and may or may not be bound to a polymer, and which can be joined together to form a hetero-cyclic system with the nitrogen, atom, n or a substituted or unsubstituted aryl radical which may or may not be bound to a polymer, n R 2 denotes a hydrogen atom, an aliphatic or cycloaliphatic radical which may be substituted or unsubstituted and saturated or unsaturated, or a substituted or unsubstituted aromatic radical, n and X denotes a halogen atom. n This process is especially useful for the synthesis of active esters of N-protected amino acids. The invention also relates to the new carbonates described above and the method of producing them, which consists in reacting an alpha-halogenated chloroformate of formula: n n R.sup.2 --CHX--O--COCl n n with an alcohol of formula R 1 OH in an inert solvent medium in the presence of an organic or inorganic base.

    专利号:US-3708477-A
    优先权日:1968-06-27
    标 题:Process of total synthesis of cephalosporin derivatives and intermediates
    发明人:MARTEL J; HEYMES R
    权利人:ROUSSEL UCLAF
    摘要:PROCESS FOR THE PREPARATION OF RACEMIC OR OPTICALLYACTIVE CEPHALOSPORINE DERIVATIVES OF THE FORMULA 2,3-(-CO-N(-R1)-CH2-),7-NH2-2-CEPHEM WHEREIN R1 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL, SUBSTITUTED AKYL, ARYL AND SUBSTITUTED ARYL, WHICH COMPRISES THE STEPS OF REACTING AN AMINO ACID OF THE FORMULA R1-NH-CH2-CH2-COOH WITH BENZYL ALCOHOL, CONDENSING THE BENZYL ESTER THUS OBTAINED WITH AN OXALATE, CONVERTING THE BENZYL ESTER OF 2,3DIOXI-4-CARBOXY-PYRROLIDINE INTO THE CORRESPONDING ACID, SUBJECTING SAID ACID TO AMINOMETHYLATION, THUS YIELDING A COMPOUND OF THE FORMULA 1-R1,3-OH,4-(R'-N(-R'')-CH2-)PYRROL-3-IN-2-ONE CONVERTING SAID COMPOUND INTO THE CORRESPONDING 4-ACYLTHIOMETHYL DERIVATIVE, CONVERTING SAID DERIVATIVE INTO THE CORRESPONDING 4-THIOMETHYL DERIVATIVE, CONDENSING SAID DERIVATIVE WITH AN ENAMINE OF THE FORMULA R-OOC-C(-Y)=CH-NH2 TO OBTAIN A THIAZINE DERIVATIVE OF THE FORMULA 2-(Y-CH(-COO-R)-),5-R1-2,3,4,5,6,7-HEXAHYDRO-PYRROLO (3,4-D)-1,3-THIAZIN-4-ONE CONVERTING SAID THIAZINE DERIVATIVE INTO A COMPOUND OF THE FORMULA 2-(H2N-CH(-COOH)-),5-R1-2,3,4,5,6,7-HEXAHYDRO-PYRROLO (3,4-)-1,3-THIAZIN-4-ONE SUBJECTING SAID COMPOUND TO THE ACTION OF A TRITYLATION AGENT, RECOVERING THE THREO ISOMER OF THE TRITYLATED DERIVATIVE, LACTAMIZING SAID THREO ISOMER TO OBTAIN THE Y-LACTAM OF DL-6H,7H-CIS-7-TRITYLAMINO-3-AMINOALKYL-CEPH 3-EME-4-CARBOXYLIC ACID, DETRITYLATING SAID Y-LACTAM AND RECOVERING SAID RACEMIC OF OPTICALLY ACTIVE CEPHALOSPORIN DERIVATIVES. THESE COMPOUNDS ARE USEFUL AS INTERMEDIATES IN THE PREPARATION OF THE CORRESPONDING 7ACYLAMINO DERIVATIVES OF THE FORMULA 2,3-(-CO-N(-R1)-CH2-),7-(R2-NH-)-2-CEPHEM WHEREIN R1 HAS THE ABOVE DEFINITION AND R2 IS THE ACYL OF AN ORGANIC CARBOXYLIC ACID WHICH COMPOUNDS ARE ALSO PART OF THE INVENTION AND ARE USEFUL AS ANTIBIOTICS.

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    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Ñacata I, Early AM, Boboy J, Neafsey DE, Sáenz FE. Effects of drug pressure and human migration on antimalarial resistance in circulating Plasmodium falciparum malaria parasites in Ecuador. Res Sq [Preprint]. 2024 Aug
    16:rs.3.rs-4638168. doi: 10.21203/rs.3.rs-4638168/v1.
    2: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Atovaquone and Proguanil. 2024 Jul 15. 10(8):2755-2774. doi: 10.1021/acsinfecdis.4c00113. Epub 2024 Jul 2. 39(22):e186. doi: 10.3346/jkms.2024.39.e186.

    合成参考文献


    参考文献:10.1155/2011/579518
    摘要:Mishra K, Dash AP, Dey N. Andrographolide: A Novel Antimalarial Diterpene Lactone Compound fromAndrographis paniculataand Its Interaction with Curcumin and Artesunate. Journal of Tropical Medicine. 2011;2011():1–6. doi: 10.1155/2011/579518.
    参考文献:10.1074/jbc.m111.269399
    摘要:Boysen KE, Matuschewski K. Arrested Oocyst Maturation in Plasmodium Parasites Lacking Type II NADH:Ubiquinone Dehydrogenase. Journal of Biological Chemistry. 2011 Sep;286(37):32661–71. doi: 10.1074/jbc.m111.269399.
    参考文献:10.1371/journal.pone.0021237
    摘要:Penna-Coutinho J, Cortopassi WA, Oliveira AA, França TCC, Krettli AU. Antimalarial Activity of Potential Inhibitors of Plasmodium falciparum Lactate Dehydrogenase Enzyme Selected by Docking Studies. PLoS ONE. 2011 Jul 14;6(7):e21237. doi: 10.1371/journal.pone.0021237.
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