2-Amino-4-chlor-1,6-dimethyl-pyridinium-iodid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 2-Amino-4-chlor-1,6-dimethyl-pyridinium-iodid
• 英文别名: 2-amino-4-chloro-1,6-dimethyl-pyrimidinium; iodide；2-Amino-4-chlor-1,6-dimethyl-pyrimidinium; Jodid；2-Amino-4-chloro-1,6-dimethylpyrimidinium iodide；4-chloro-1,6-dimethylpyrimidin-1-ium-2-amine;iodide
• 化学式: C₆H₉ClN₃*I
• 分子量: 285.515
• InChiKey: SVWHYPUEEAXFGA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.55
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  42.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-Amino-4-chlor-1,6-dimethyl-pyridinium-iodid 在 盐酸 、 水 作用下， 生成 1,6-Dimethyl-N⁷-phenylcytosin
  参考文献：
  名称：

  The Effects of Membership in Church-Related Associations and Labor Unions on Age Differences in Voluntary Association Affiliations

  摘要：

  目的：当年龄组之间的构成差异受到控制时，自愿协会会员资格中年龄差异的二元曲线模式将被一种会员水平峰值出现在中年后期并在此后保持相对稳定的模式所取代。我们试图确定当两类协会的广泛会员资格被取消时，这种调整后的模式是否仍然存在：（1）与教会相关的组织，其中会员资格随着年龄的增长而增加，但可能与教会会员资格本身相混淆； (2) 工会，其成员资格也很广泛，但可能不是“自愿的”。 设计和方法：使用 1974 年至 1994 年间进行的 12 次全国性调查的汇总数据对 14 类协会的总成员资格进行了审查。双变量水平上出现了熟悉的曲线关系，但在多变量分析中，会员水平从 18-24 岁上升到 55-59 岁，并在 85 岁及以上一直保持接近该水平。 意义：结果再次证实，自愿协会中的年龄差异隶属关系是由于年龄构成差异造成的；然而，它们也表明，通过控制观察到的模式既不是由与教会有关的"协会"的成员资格所驱动的，也不是因为工会成员资格被排除在外而改变的。

  DOI：

  10.1093/geront/41.2.250
• 作为产物：
  描述：

  2-氨基-4-氯-6-甲基嘧啶 、 对甲苯磺酸甲酯 在 sodium iodide 作用下， 生成 2-Amino-4-chlor-1,6-dimethyl-pyridinium-iodid
  参考文献：
  名称：

  DE823452

  摘要：

  公开号：

文献信息

• Trypanocide Diamidine mit drei Ringen in zwei isolierten Ringsystemen
  作者：Otto Dann、Rainer Fernbach、Wolfgang Pfeifer、Ekke Demant、Gerhard Bergen、Siegfried Lang、Gerd Lürding

  DOI：10.1002/jlac.19727600105

  日期：1972.9.29

  Es werden Diamidine synthetisiert, welche sich vom Typ A des 6- oder 5-Amidino-2-[4-amidino-phenyl]-thionaphthens oder -benzofurans dadurch ableiten, daß der annelierte Fünfring weiter variiert wird, daß ein- und zweigliedrige Brücken zwischen die beiden Ringsysteme eingeschoben werden, und daß die flankierenden Amidino-Gruppen abgewandelt werden. – Nur bei 5-Amidino-2-[4-amidino-phenyl]-indazol (4c)

  Es werden Dimidine synthetistisiert，welche sich vom Typ A des 6-oder 5-Amidino-2- [4-amidino-phenyl] -thionaphthens oder -benzofurans dadurchableiten，daßder annelierteFünfringweiter variiert wird，daßein-e- und-rigund贝尔登（Ringsysteme）音响系统公司和弗拉基耶伦登（Fankierenden）大街上的阿米迪诺-格鲁彭（Amidino-Gruppen）abgewandelt werden。– Nur bei 5-Amidino-2- [4-amidino-phenyl] -indazol（4c）和-benztriazol（10d）漂白剂Hervorragenden trypanociden
• Pyrimidine derivatives
  申请人：Imperial Chemical Industries Plc

  公开号：US05223505A1

  公开（公告）日：1993-06-29

  This invention concerns novel aminopyrimidinium salts of the formula I: ##STR1## in which R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkyl-alkyl; one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl, alkenyl, alkoxyalkyl, phenyl, phenylalkyl, cycloalkyl or cycloalkyl-alkyl; or both of R.sup.2 and R.sup.6 are basic groups as mentioned above; and R.sup.5 is hydrogen, (1-4C)alkyl or (3-6C)alkenyl; or R.sup.2 is a basic group as mentioned above, and R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyrimidine ring, complete a benzene ring; R.sup.4 is hydrogen, alkyl, cycloalkyl-alkyl, alkenyl, alkynyl or phenylalkyl; or R.sup.4 is an optionally substitutued alkylene or alkenylene linked to the nitrogen atom of the group Q.A.N--, either of which linking groups may thereby completing a ring including two adjacent carbon atoms of Q, the carbon atoms of A and the adjacent nitrogen atom of the group --A.N--; A is a direct bond to the the group --N(R.sup.4)-- or is alkylene or oxyalkylene; Q is a pyridyl, furyl, thienyl or phenyl moiety; and Y is a physiologically acceptable anion; but excluding a number of compounds specified hereinafter. The invention also includes certain closely related anhydro-base derivatives which, like the formula I compounds, possess beneficial effects on the cardiovascular system (and in particular beneficial effects modulated via the sino-atrial node). Also included are pharmaceutical compositions containing the formula I compound (or a related anhydro-base) as active ingredient, and processes for the manufacture of the various novel compounds.

  这项发明涉及式I的新型氨基嘧啶盐：其中R.sup.1是烷基，烯烃基，环烷基，苯基，苯基烷基或环烷基-烷基；R.sup.2和R.sup.6中的一个是从氨基，烷基氨基，最多含有八个碳原子的二烷基氨基，吡咯啉基，哌啶基和吗啉基中选择的一种碱性基团；而另一个是氢，烷基，烯烃基，烷氧基烷基，苯基，苯基烷基，环烷基或环烷基-烷基；或者R.sup.2和R.sup.6都是上述提到的碱性基团；R.sup.5是氢，（1-4C）烷基或（3-6C）烯烃基；或者R.sup.2是上述提到的碱性基团，而R.sup.5和R.sup.6一起形成亚烷基或者与嘧啶环的附加碳原子一起形成苯环；R.sup.4是氢，烷基，环烷基-烷基，烯烃基，炔烃基或苯基烷基；或者R.sup.4是可选取代的烷基或烯基与Q.A.N--基团的氮原子相连，这些连接基团可能形成包括Q的两个相邻碳原子，A的碳原子和--A.N--基团的相邻氮原子的环；A是直接连接到--N(R.sup.4)--基团的键或者是烷基或氧基烷基；Q是吡啶基，呋喃基，噻吩基或苯基基团；Y是生理上可接受的阴离子；但不包括下文中指定的一些化合物。该发明还包括某些紧密相关的无水碱衍生物，类似于式I化合物，对心血管系统具有有益效果（尤其是通过窦房结调节的有益效果）。还包括含有式I化合物（或相关的无水碱）作为活性成分的药物组合物，以及用于制造各种新型化合物的方法。
• Quaternary salts of pyrimidylaminoquinolines
  申请人：ICI LTD

  公开号：US02585905A1

  公开（公告）日：1952-02-19

  Mono- and di-quaternary salts of pyrimidylaminoquinolines, possessing trypanocidal activity and of the general formula Pq-NH-A, (wherein P represents a 2-, 4- (or 6-) amino-substituted pyrimidine nucleus which is attached to the -NH- linkage at another of the 2-, 4- (or 6-) positions and which may be further substituted in the remaining 2-, 4- (or 6-) position by an alkyl radical of not more than 5 carbon atoms or an amino group, A represents Q or Qq where Q is a quinoline nucleus which is substituted in the 2- or 4- position by an amino group and may be further substituted by an alkyl group of not more than 5 carbon atoms, and which bears the linking-NH- group in the 6-position, and the symbols q indicate that the preceding nuclei P and Q respectively are in the form of their quaternary salts), or tantomeric forms thereof, are manufactured by reacting a compound of the formula PqX (wherein X represents a halogen atom or a group -SR, R being a hydrocarbon radical, obtainable by the process of Specification 634,471) with a compound of the formula NH2A, or a salt thereof, or a substance which will give rise thereto under the reaction conditions (e.g. an acyl derivative thereof). The reaction may be effected by heating the reactants together, advantageously in a liquid medium and in the presence of an acid. In examples: (1) 2 - chloro - 4 - methyl - 6 - aminopyrimidine 3-methiodide is boiled with 4 : 6-diaminoquinaldine methochloride in dilute hydrochloric acid to produce 4-amino-6-(61-amino - 41 - methylpyrimidyl - 21 - amino) - quinaldine 1 : 31-dimethiodide; (2) 4-chloro-2-amino-6-methylpyrimidine 1-methiodide is boiled in water with 4 : 6-diaminoquinaldine methochloride hydrochloride, yielding 4-amino-6-(21-amino-61-methylpyrimidyl-41-amino) p -quinaldine 1 : 11-dimethiodide, or the tantomeric 4-amino-6-(21-imino-11 : 61-dimethyl-11 : 21-dihydropyrimidyl-41-amino)-quinaldine 1-methiodide hydriodide or 4-imino-1-methyl-6-(21-amino-61-methylpyrimidyl -41-amino)-1 : 4-dihydroquinaldine 11-methiodide hydriodide or 4-imino-1-methyl-6-(21-imino-11 : 61-dimethyldihydropyrimidyl-41-amino)-1 : 4-dihydroquinaldine dihydriodide; the product may be converted into the dimethochloride by treating an aqueous solution thereof with hydrochloric acid or sodium chloride, or into the dimethobromide by analogous treatment; (3) the pyrimidine reactant in (2) is replaced by 4-iodo-2-amino-6-methylpyrimidine 3-methiodide, producing the corresponding 1 : 31-dimethiodide, which may be converted with silver chloride into the dimethochloride and with sodium carbonate solution into 4-amino-6-(21-imino-31 : 61-dimethyl-2 : 3-dihydropyrimidyl-41-amino)-quinaldine 1-methiodide; (4) 4 : 6-diaminoquinaldine methochloride is heated with 2-amino-4-methylthio6-methylpyrimidine 1-methiodide to give the product of (2); (5) the quinaldine reactant in (3) is replaced by 4 : 6-diaminoquinaldine methiodide; (6) the pyrimidine reactant in (5) is replaced by 4-chloro-2 : 6-diaminopyrimidine 3-methiodide, and (7) by the corresponding 1-methiodide; (8) 4 : 6-diaminoquinoline methiodide is reacted as in (2); (9) the quinaldine reactant of (2) is replaced by 2 : 6-diaminolepidine methiodide; (10) 4-amino-6-acetylaminoquinaldine 1-metho-methylsulphate and 4-chloro-2-amino-6-methylpyrimidine 1-methomethylsulphate are reacted as in (1) and the product is treated with hydrochloric acid to give the dimethochloride of (2); (11) the pyrimidine reactant of (10) is replaced by the 1-methiodide; (12) 4 : 6-diaminoquinaldine and 4-chloro-2 : 6-diaminopyrimidine 3-methiodide are reacted as in (1) to produce 4-amino-6-(21 : 61-diaminopyrimidyl-41-amino)-quinaldine 31-methiodide hydriodide; (13) 4 : 6 - diaminoquinaldine ethiodide is reacted as in (2). Specification 634,531 also is referred to. 4 : 6-Diaminoquinaldinium salts.-The methochloride hydrochloride is obtainable by treating 4-amino-6-acetylaminoquinaldine with dimethyl sulphate in nitrobenzene and refluxing the product with aqueous hydrochloric acid. It may be converted into the methochloride by the action of sodium carbonate solution and into the methiodide by the action of a solution of sodium carbonate and excess of potassium iodide. The ethiodide is obtainable by treating 4-amino-6-acetylaminoquinaldine with diethyl sulphate in nitrobenzene, treating the product with sodium iodide solution, hydrolysing with hydrochloric acid and adding sodium carbonate and sodium iodide. 4 : 6-Diaminoquinoline methiodide is obtainable from ethyl 6-acetylamino-4-hydroxyquinoline-2-carboxylate by saponification, decarboxylation, treatment with phosphorous oxychloride and then with ammonia in the presence of phenol, quaternation of the resulting 4-amino-6-acetylaminoquinoline by means of dimethyl sulphate in nitrobenzene, hydrolysis with hydrochloric acid and treatment with sodium carbonate and sodium iodide. 2 : 6-Diaminolepidine methiodide is obtainable from 2-chloro-6-nitrolepidine by treatment with ammonia in the presence of phenol and acetamide, quaternation with dimethyl sulphate in nitrobenzene, treatment with excess of sodium chloride, reduction of the nitro group with iron and methanolic hydrochloric acid and treatment with sodium carbonate and sodium iodide.

  具有抗锥虫活性的嘧啶基氨基喹啉的单、双季铵盐，其一般式为Pq-NH-A（其中P代表2-、4-（或6-）氨基取代的嘧啶核，该核附着在另一个2-、4-（或6-）位置的-NH-连接处，并且在其余的2-、4-（或6-）位置上可能进一步取代为不超过5个碳原子的烷基或氨基，A代表Q或Qq，其中Q是一个喹啉核，在2-或4-位置上被氨基取代，并且可能进一步被不超过5个碳原子的烷基取代，其在6-位置带有连接-NH-基团，符号q表示前面的核P和Q分别以其季铵盐的形式存在，或其异构体，可以通过将公式PqX（其中X代表卤素原子或由规范634,471的过程获得的-SR基团，其中R是一个碳氢基团）与公式NH2A或其盐或在反应条件下将产生该物质的物质（例如，其酰基衍生物）反应制备。反应可以通过加热反应物一起进行，优选在液体介质中，在酸的存在下进行。在例子中：（1）2-氯-4-甲基-6-氨基嘧啶3-碘化物在稀盐酸中与4：6-二氨基喹啉甲基氯化物沸腾，产生4-氨基-6-（6-氨基-4-甲基嘧啶-2-氨基）-喹啉1：3-二碘化物；（2）4-氯-2-氨基-6-甲基嘧啶1-碘甲烷酸盐在水中与4：6-二氨基喹啉甲基氯化物盐酸盐沸腾，产生4-氨基-6-（2-氨基-6-甲基嘧啶-4-氨基）-喹啉1：1-二碘化物，或其异构体4-氨基-6-（2-亚氨基-1，1：6，1-二甲基-2，3-二氢嘧啶-4-氨基）-喹啉1-碘甲烷酸盐，或4-亚氨基-1-甲基-6-（2-氨基-6-甲基嘧啶-4-氨基）-1：4-二氢喹啉11-碘甲烷酸盐，或4-亚氨基-1-甲基-6-（2-亚氨基-1，1：6，1-二甲基嘧啶-4-氨基）-1：4-二氢喹啉二碘化物；可以通过用盐酸或氯化钠处理其水溶液将产物转化为二甲基氯化物或类似处理将其转化为二甲基溴化物；（3）（2）中的嘧啶反应物被4-碘-2-氨基-6-甲基嘧啶3-碘甲烷酸盐所取代，产生相应的1：3-二碘化物，该化合物可以与氯化银转化为二甲基氯化物，或与碳酸钠溶液转化为4-氨基-6-（2-亚氨基-3,1：6,1-二甲基嘧啶-4-氨基）-喹啉1-碘甲烷酸盐；（4）4：6-二氨基喹啉甲基氯化物与2-氨基-4-甲硫基-6-甲基嘧啶1-碘甲烷酸盐加热，产生（2）的产物；（5）（3）中的喹啉反应物被4：6-二氨基喹啉甲烷酸盐所取代；（6）（5）中的嘧啶反应物被4-氯-2：6-二氨基嘧啶3-碘甲烷酸盐所取代，（7）被相应的1-碘甲烷酸盐所取代；（8）4：6-二氨基喹啉甲烷酸盐如（2）中所述反应；（9）（2）中的喹啉反应物被2：6-二氨基乙二噻啶甲烷酸盐所取代；（10）4-氨基-6-乙酰氨基喹啉1-甲硫酸盐和4-氯-2-氨基-6-甲基嘧啶1-甲硫酸盐如（1）中所述反应，产物用盐酸处理后得到（2）的二甲基氯化物；（11）（10）中的嘧啶反应物被1-甲烷基碘化物所取代；（12）4：6-二氨基喹啉和4-氯-2：6-二氨基嘧啶3-碘甲烷酸盐如（1）中所述反应，产生4-氨基-6-（2：4-二氨基嘧啶-6,1-二氨基）-喹啉3-碘甲烷酸盐；（13）4：6-二氨基喹啉乙碘化物如（2）中所述反应。规范634,531也被提到。4：6-二氨基喹啉盐-甲基氯化物盐酸盐可以通过将4-氨基-6-乙酰氨基喹啉与硫酸二甲酯在硝基苯中处理，并将产物与水合盐酸回流处理得到。它可以通过钠碳酸溶液的作用转化为甲基氯化物，通过钠碘化物溶液和过量的碘化钾的作用转化为甲基碘化物。乙碘化物可以通过将4-氨基-6-乙酰氨基喹啉与硫酸二乙酯在硝基苯中处理，用碘化钠溶液处理产物，水解并加入碳酸钠和碘化钠得到。4：6-二氨基喹啉甲烷酸盐可以通过将乙基6-乙酰氨基-4-羟基喹啉-2-羧酸酯皂化、脱羧、用氯化亚磷酰处理，然后在苯酚存在下与氨一起处理，用硝基苯中的二甲基硫酸盐季铵化得到4-氨基-6-乙酰氨基喹啉，用盐酸水解并用碳酸钠和碘化钠处理得到。2：6-二氨基乙二噻啶甲烷酸盐可以通过用苯酚和乙酰胺处理2-氯-6-硝基乙二噻啶，用硝基苯中的二甲基硫酸盐季铵化，过量的氯化钠处理，铁和甲醇盐酸还原硝基基团，然后用碳酸钠和碘化钠处理得到。
• Process for the manufacture of diquaternary salts of pyrimidylaminoquinolines
  申请人：MURIEL RUTH CURD

  公开号：US02585972A1

  公开（公告）日：1952-02-19

  Quaternary salts of pyrimidylaminoquinolines in which either the 2-position of the pyrimidine nucleus or the 4-position of the quinoline nucleus, or both, are substituted by an amino- or lower alkylamino-group, the -NH- linking is in the 4 : 61-positions respectively, and each nucleus may be optionally substituted by alkyl groups, are obtained by heating the quaternary compound bearing ether and/or thioether groups in the above-mentioned 2- and/or 4-positions with ammonia or lower alkylamines in a solvent. In examples, pyrimidylaminoquinoline quaternary salts having methyl thio-, or benzylthio in the 2-pyrimidyl, and 4-quinoline, positions, and/or having methoxy, ethoxy, or phenoxy in the 4-quinoline position, with amino and methyl groups as other substituents are converted into the corresponding amine or alkylamine with ammonia or ethylamine in various solvents. There is described also the preparation, as starting materials, of the quaternary satls of pyrimidylamino-quinolines substituted as required above by amino, and methyl groups and having methylthio, benzylthio, alkoxy or phenoxy groups in the required positions by the condensation of the corresponding halogenated pyrimidine ether or thioether with an aminoquinoline, or the halogenated pyrimidine with an aminoquinoline ether or thioether, non-reacting amino groups being acetylated and later hydrolysed, if necessary, and with intermediate or subsequent conversion to the quaternary salts. 6-Acetylamino and 6-amino-4-methyl, 4-benzylthio-ethers, or 4-methyl, ethyl and phenyl ethers of quinoline or quinaldine are obtained by the action of the corresponding mercaptan-, alcohol- or phenol-sodium salt or a mixture producing these, on the 4-halogen- or 4-hydroxy-quinoline compound, followed if necessary by hydrolysing the acetylamino-group. Specifications 634,531, 634,818, 658,203 and 658,204 are referred to.

  2-吡咯啉基氨基喹啉的第四价盐，在其中吡咯啉核的2-位置或喹啉核的4-位置或两者都被氨基或较低的烷基氨基取代，-NH-连接分别在4:6或1-位置，每个核也可以选择性地被烷基取代。通过在溶剂中用氨或较低的烷基胺加热带有醚和/或硫醚基团的第四价化合物，可以获得这些盐。例如，具有2-吡咯啉中甲硫基或苄基硫基和4-喹啉位置的吡咯啉基氨基喹啉四价盐，并/或具有4-喹啉位置的甲氧基、乙氧基或苯氧基，具有氨基和甲基基团作为其他取代基的盐，可以用氨或乙基胺在各种溶剂中转化为相应的胺或烷基胺。还描述了作为起始材料的吡咯啉基氨基喹啉的第四价盐，这些盐如上所述被氨基和甲基基团取代，并在所需位置具有甲硫基、苄基硫基、烷氧基或苯氧基，通过相应卤代吡咯啉醚或硫醚和氨基喹啉的缩合或卤代吡咯啉和氨基喹啉醚或硫醚，非反应性氨基被乙酰化，如果需要，后来水解，并通过中间或后续转化成第四价盐。通过在4-卤代或4-羟基喹啉化合物上作用相应的巯基醇盐、醇盐或酚盐或产生这些的混合物，然后如有必要水解乙酰氨基基团，可以获得6-乙酰氨基和6-氨基-4-甲基、4-苄基硫醚、或4-甲基、乙基和苯基醚的喹啉或喹啉醛醚。参考规范634,531、634,818、658,203和658,204。
• Process for preparing diquaternary salts of pyrimidylamino quinolines
  申请人：MURIEL RUTH CURD

  公开号：US02585910A1

  公开（公告）日：1952-02-19

  Di-quaternary salts of pyrimidylamino-quinolines having trypanodical properties are obtained by treating a pyrimidylamino-quinoline in which either the pyrimidine or the quinoline compound is in the form of a quaternary salt, and may be as described below, with a quaternary salt forming agent, such as methyl iodide, dimethyl sulphate and methyl p-toluene sulphonate. In the examples the pyrimidine nucleus is substituted in the 2-, 4- (or 6-) position by lower alkylamino, e.g. methyl-, and isopropylamino, or amino-groups, in another of these positions by a lower alkyl radical, e.g. methyl, or amino, or a lower alkylamino group, and is attached to the linking -NH- group at the remaining 2-, 4-(or 6-) positions, while the quinoline nucleus is substituted in the 4-position by an amino- or lower alkylamino-group, e.g. methylamino-, ethylamino-, and further by a lower alkyl group or groups, e.g. 2-methyl, and bears the linking -NH- group in the 6-position. If the 4-substituent in the quinoline nucleus is not lower alkylamino-, the pyrimidine nucleus must contain a lower alkylamino-group. The di-quaternary salts described include methiodides, and metho - p - toluene sulphonates, mostly being converted ultimately into the former, from other intermediate quaternary salts, such as the methyl sulphate. Pyrimidylaminoquinolines and their monoquaternary salts used as initial materials, substituted as described, may be obtained by condensing a suitably substituted 6-amino-quinoline or its quaternary salt with a 4-chloro-pyrimidine or its quaternary salt dehydrating the monohydrate obtained if necessary, and replacing the quaternary group if required, e.g. the hydriodides to the methiodides. 4-Methyl and ethyl-amino-6-aminoquinolines are obtained by hydrolysis of the N-acetyl derivatives. Specification 658,203 is referred to.

  通过用季铵盐形成剂（例如甲基碘化物、二甲基硫酸酯和对甲苯磺酸甲酯等）处理含有三联氮嘧啶基氨基喹啉的化合物，可以制备具有抗锥虫作用的嘧啶基氨基喹啉的二季铵盐。在这些化合物中，三联氮嘧啶或喹啉化合物中的一个以季铵盐的形式存在，例如在2-、4-（或6-）位上被较低的烷基氨基（例如甲基和异丙基氨基）或氨基基团取代，在另一个这些位置上，被较低的烷基（例如甲基）或氨基基团或较低的烷基氨基取代，并与剩余的2-、4-（或6-）位上的连接-NH-基团相连。同时，喹啉核在4-位上被氨基或较低的烷基氨基（例如甲基氨基和乙基氨基）取代，进一步被较低的烷基或烷基组取代（例如2-甲基），并在6-位上带有连接-NH-基团。如果喹啉核中的4-取代基不是较低的烷基氨基，则三联氮嘧啶核必须包含较低的烷基氨基基团。所述的二季铵盐包括甲碘酸盐和甲基对甲苯磺酸盐，大多数最终转化为前者，从其他季铵盐中间体（例如甲基硫酸盐）中得到。作为初始材料使用的嘧啶基氨基喹啉及其单季铵盐，可以通过将适当取代的6-氨基喹啉或其季铵盐与4-氯嘧啶或其季铵盐缩合，必要时脱水得到单水合物，并在需要时替换季铵基团，例如从氢碘酸盐替换为甲碘酸盐。4-甲基和乙基氨基-6-氨基喹啉可以通过水解N-乙酰衍生物获得。参考规范658,203。