hydrogen maleate ion | 18610-42-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: hydrogen maleate ion
• 英文别名: Hydrogen maleate；(Z)-4-hydroxy-4-oxobut-2-enoate
• CAS: 18610-42-9
• 化学式: C₄H₃O₄
• 分子量: 115.065
• InChiKey: VZCYOOQTPOCHFL-UPHRSURJSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  8
• 可旋转键数：
  1
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  77.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  benzyl-(5-methyl-7-propyl-1(3),4-dihydro-imidazo[5,1-f][1,2,4]triazin-2-yl)-amine 、 hydrogen maleate ion 生成 benzyl-(5-methyl-7-propyl-imidazo[5,1-f][1,2,4]triazin-2-yl)-amine
  参考文献：
  名称：

  Imidazo [5,1-f]-as-triazines

  摘要：

  通式为##SPC1##的化合物：其中，R.sub.1和R.sub.2可能相同也可能不同，代表氢原子或烷基，该烷基可以被芳基取代，或代表烷酰基，芳酰基或烷基磺酰基；R.sub.3代表氢原子，或烷基，该烷基可以被芳基取代，或代表烯基，芳基或烷硫基；R.sub.4代表氢原子或烷基；R.sub.5代表氢原子或芳基或烷基，该烷基可以被环烷基取代；以及生理上可接受的盐和衍生物，以及由亲核加成形成的加成物。这些化合物作为平滑肌松弛剂和磷酸二酯酶抑制剂，并具有心脏强心和利尿作用。它们也用于治疗皮肤疾病和痛风。

  公开号：

  US03941785A1
• 作为产物：
  描述：

  顺丁烯二酸 以 乙醚 、 乙酸乙酯 为溶剂， 生成 hydrogen maleate ion
  参考文献：
  名称：

  Dithienylalkylamines and process for their production

  摘要：

  有一些化合物的配方为 ##STR1## 其中 >A--B-- 可以是 >C(OH)--CH.sub.2 -- 或 >C.dbd.CH，Alk 是一条直链或支链的 C.sub.1 -C.sub.5 烷基链，-NHY 是 ##STR2## 其中 R' 是氢、苯基、一次或两次被 C.sub.1 -C.sub.4 烷基、C.sub.1 -C.sub.4 烷氧基或卤素原子取代的苯基、C.sub.1 -C.sub.6 烷基、C.sub.1 -C.sub.4 羟基烷基或烷基部分由1-4个碳原子组成的苯基烷基或包含1至3个C.sub.1 -C.sub.4 烷氧基取代基的苯基烷基。这些化合物对改善周围和脑循环有效。还可以制备配方为(II)的中间化合物，其中 NHY 被氯、溴或碘取代。

  公开号：

  US04206213A1
• 作为试剂：
  描述：

  2-甲硫基-2-咪唑啉 、 N-(cyclopropylmethyl)isatoic anhydride 、 sodium hydroxide 、 1,4-二氧六环 在 二氯甲烷 、 盐酸 、 乙醚 、 水 、 Sodium sulfate-III 、 正戊烷 、 hydrogen maleate ion 作用下， 反应 1.0h， 以to obtain 10-cyclopropylmethyl-2,3-dihydroimidazo[2,1-b]quinazolin-5(10H)-one hydrogen maleate, m.p. 189°-192°C.的产率得到10-cyclopropylmethyl-2,3-dihydro-imidazo[2,1-b]quinazolin-5(10H)-one maleate
  参考文献：
  名称：

  Pharmacologically active tricyclic quinazolinones

  摘要：

  这些化合物是具有生物活性的三环喹唑啉类化合物，属于咪唑[2,1-b]喹唑啉-5-酮，嘧啶并[2,1-b]喹唑啉-6-酮和二氮杂[2,1-b]喹唑啉-7-酮类，例如作为支气管扩张剂。制备这些化合物的过程包括将N-羧基蒽醌酐（异香草酸酐）与环状伪硫脲反应，如2-有机硫醇基-4,5-二氢咪唑或2-有机硫醇基-3,4,5,6-四氢嘧啶。

  公开号：

  US03969506A1

文献信息

• Tricyclic compounds
  申请人：SPOFA, spojene podniky pro zdravotnickou vyrobu

  公开号：US04431808A1

  公开（公告）日：1984-02-14

  A technique is described for the preparation of a wide variety of basic derivatives of linearly condensed tricyclic systems formed by two external benzene nuclei and a 7-membered central ring having 2 chalcogen atoms as hetero atoms. Derivatives of 11H-dibenzo(b,e)-1,4-dioxepin are obtained when the chalcogens are both oxygen atoms; derivatives of 11H-dibenzo(b,f)-1,4-dithiepin are obtained when the chalcogens are both sulfur atoms; derivatives of 6H-dibenz(b,e)-1,4-oxathiepin and 11H-dibenz(b,f)-1,4-oxathiepin are obtained with combinations of sulfur and oxygen atoms as chalcogens.

  描述了一种技术，用于制备由两个外部苯核和一个具有2个硫族元素原子作为杂原子的7-成员中心环形成的线性紧凑三环系统的各种基本衍生物。当硫族元素均为氧原子时，得到11H-二苯并(b,e)-1,4-二氧杂环己烷的衍生物；当硫族元素均为硫原子时，得到11H-二苯并(b,f)-1,4-二硫杂环己烷的衍生物；当硫族和氧族元素的组合作为硫族元素时，得到6H-二苯并(b,e)-1,4-氧硫杂环己烷和11H-二苯并(b,f)-1,4-氧硫杂环己烷的衍生物。
• Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine
  申请人：SPOFA, United Pharmaceutical Works

  公开号：US04238611A1

  公开（公告）日：1980-12-09

  Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine and processes for the preparation thereof are described. The compositions evidence psychotropic and antimicrobial characteristics and are of low toxicity. The described compounds are of the general formula ##STR1## wherein R.sup.2, R.sup.3, R.sup.7 and R.sup.8 are selected from among hydrogen, fluorine and chlorine atoms, a fluoromethyl group, a methoxy group and a hydroxyl group, at least three of R.sup.2, R.sup.3, R.sup.7 and R.sup.8 being other than hydrogen, R being selected from among hydrogen, alkyl or alkylhydroxy groups having from 1-3 carbon atoms, an acyloxyalkyl group having from 8-10 carbon atoms in the acyl moiety and from 2-3 carbon atoms in the alkyl moiety and an ethoxycarbonyl group, m and n representing integers from 0-1 and the bond between the 10 and 11 carbon atoms being either a single or double bond.

  描述了10-哌嗪二苯并(b,f)噻吩的多取代衍生物及其制备方法。这些化合物具有精神药理和抗微生物特性，毒性低。所描述的化合物为一般式##STR1## 其中R.sup.2、R.sup.3、R.sup.7和R.sup.8从氢、氟和氯原子、氟甲基基团、甲氧基和羟基中选择，至少三个R.sup.2、R.sup.3、R.sup.7和R.sup.8不是氢，R从氢、烷基或具有1-3个碳原子的烷基羟基基团、在酰基中具有8-10个碳原子，在烷基中具有2-3个碳原子和乙氧羰基中选择，m和n代表0-1的整数，10和11碳原子之间的键为单键或双键。
• Tetrafluorophenethylaralkylamine compounds
  申请人：Merck & Co., Inc.

  公开号：US03978127A1

  公开（公告）日：1976-08-31

  New fluoro derivatives of aralkylamine compounds, particularly 2-(2-phenyl-1,1,2,2-tetrafluoroethyl)benzylamine, as well as the N-alkyl and the N,N-dialkyl derivatives thereof are prepared by reaction of 2-bromobenzonitrile with benzylmagnesium chloride to produce 2'-bromo-2-phenylacetophenone; oxidation of said acetophenone with selenous acid to produce 2-bromobenzil; conversion of the benzil compound by treatment with sulfur tetrafluoride to the corresponding 2-bromo-.alpha. ,.alpha.-.alpha.',.alpha.'-tetrafluorobibenzyl; followed by reaction of the 2-bromobibenzyl compound with a metal cyanide to produce the corresponding 2-(2-phenyl-1,1,2,2-tetrafluoroethyl)benzonitrile. This nitrile compound is then reduced with lithium aluminum hydride to produce the corresponding benzylamine, which is then converted, if desired, to the N-alkyl and/or N,N-dialkyl 2-(2-phenyl-1,1,2,2-tetrafluoroethyl)benzylamine. Alternatively, the nitrile or the precursor bromobibenzyl can be converted by Grignard reactions to the corresponding .alpha.-alkyl or .alpha.,.alpha.-dialkylbenzylamine which can then be converted if desired to the corresponding N-alkyl and/or N,N-dialkyl substituted benzylamine compound. The phenyltetrafluoroethylbenzylamine as well as its N-alkyl and N,N-dialkyl derivatives are active as antiarrhythmic agents.

  新的氟代取代的芳基胺化合物，特别是2-(2-苯基-1,1,2,2-四氟乙基)苄胺，以及其N-烷基和N,N-二烷基衍生物，通过2-溴苯甲腈与苄基氯化镁反应制备2'-溴-2-苯基乙苯酮；将该乙苯酮氧化为硒酸，生成2-溴苯甲醛；通过硫四氟化物处理苯甲醛化合物，转化为相应的2-溴-α,α,α',α'-四氟联苯；然后将2-溴联苯化合物与金属氰化物反应，产生相应的2-(2-苯基-1,1,2,2-四氟乙基)苯甲腈。然后，将这种腈化合物还原为相应的苄胺，然后转化为必要时的N-烷基和/或N,N-二烷基2-(2-苯基-1,1,2,2-四氟乙基)苄胺。或者，腈或前体溴联苯可以通过格氏试剂反应转化为相应的α-烷基或α,α-二烷基苄胺，然后如果需要，可以转化为相应的N-烷基和/或N,N-二烷基取代的苄胺化合物。苯基四氟乙基苄胺以及其N-烷基和N,N-二烷基衍生物作为抗心律失常药物具有活性。
• (4-Hydroxy-4-piperidyl)-alkanoic acid amides
  申请人：Sandoz Ltd.

  公开号：US04178377A1

  公开（公告）日：1979-12-11

  The present invention concerns novel compounds of formula I, ##STR1## wherein R.sub.1 is phenethyl, phenethyl monosubstituted in the phenyl ring by fluorine, chlorine, bromine, lower alkyl or lower alkoxy, butyrophenone or butyrophenone monosubstituted in the phenyl ring by fluorine, chlorine, bromine, lower alkyl or lower alkoxy, R.sub.2 is an OR.sub.5 group, wherein R.sub.5 is lower alkyl, lower alkenyl, phenyl or phenyl monosubstituted by fluorine, chlorine, bromine, lower alkyl or lower alkoxy, or an ##STR2## group, wherein independently each of R.sub.6 and R.sub.7 is hydrogen, lower alkyl or cycloalkylalkyl, cycloalkyl, phenyl, phenyl monosubstituted by fluorine, chlorine, bromine, lower alkyl or lower alkoxy, lower phenylalkyl or lower phenylalkyl monosubstituted in the phenyl ring by fluorine, chlorine, bromine, lower alkyl or lower alkoxy, or wherein R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bound, form a saturated heterocycle of 5 to 6 ring members, which may optionally contain as second hetero atom oxygen, sulphur or nitrogen substituted by lower alkyl, R.sub.3 is lower alkyl or cycloalkylalkyl, cycloalky, phenyl or phenyl monosubstituted by fluorine, chlorine, bromine, lower alkyl or lower alkoxy, or when R.sub.1 is phenethyl or phenethyl monosubstituted in the phenyl ring by fluorine, chlorine, bromine, lower alkyl or lower alkoxy, alternatively lower alkenyl, and R.sub.4 is hydrogen or lower alkyl, or R.sub.3 and R.sub.4 together with the carbon atom to which they are bound form a cycloalkyl ring of 4 to 6 carbon atoms, and analgesic pharmaceutical composition containing the compounds.

  本发明涉及公式I的新化合物，其中R.sub.1是苯乙基，苯乙基在苯环上单取代为氟、氯、溴、低碳烷基或低碳基氧，丁酰苯酮或丁酰苯酮在苯环上单取代为氟、氯、溴、低碳烷基或低碳基氧，R.sub.2是OR.sub.5基团，其中R.sub.5是低碳烷基、低碳烯基、苯或苯单取代为氟、氯、溴、低碳烷基或低碳基氧，或者是##STR2##基团，其中独立的R.sub.6和R.sub.7中的每一个是氢、低碳烷基或环烷基烷基、环烷基、苯、苯单取代为氟、氯、溴、低碳烷基或低碳基氧、低苯基烷基或低苯基烷基在苯环上单取代为氟、氯、溴、低碳烷基或低碳基氧，或者R.sub.6和R.sub.7与它们连接的氮原子一起形成有5到6个环成员的饱和杂环，该环可以选择性地包含第二个杂原子氧、硫或氮，被低碳基取代的R.sub.3是低碳烷基或环烷基烷基、环烷基、苯或苯单取代为氟、氯、溴、低碳烷基或低碳基氧，或者当R.sub.1是苯乙基或苯乙基在苯环上单取代为氟、氯、溴、低碳烷基或低碳基氧时，也可以是低碳烯基，R.sub.4是氢或低碳烷基，或者R.sub.3和R.sub.4与它们连接的碳原子一起形成有4到6个碳原子的环烷基环，以及含有这些化合物的镇痛药物组成。
• Phenylvinyl morpholine compounds
  申请人：Imperial Chemical Industries Limited

  公开号：US04010266A1

  公开（公告）日：1977-03-01

  Morpholine derivatives, typically those of the formula: ##STR1## wherein A is an ethylene or vinylene radical and X is a phenyl radical optionally substituted by one or two substituents selected from halogen atoms, alkyl and alkoxy radicals of 1 to 6 carbon atoms and aryloxy radicals of 1 to 6 carbon atoms, the aryloxy radicals themselves being optionally substituted by one or two substituents selected from halogen atoms and alkyl radicals of 1 to 4 carbon atoms, and the pharmaceutically-acceptable acid-addition salts thereof. Processes for making these compounds, pharmaceutical compositions containing them and a method of restoring to normal abnormal mental states in warm-blooded animals are also disclosed.

  Morpholine衍生物，通常是以下公式的衍生物：## STR1 ## 其中A是一个乙烯或乙烯基基团，X是一个苯基基团，可选地被一个或两个取代基取代，所述取代基选自卤素原子，1至6个碳原子的烷基和烷氧基以及1至6个碳原子的芳氧基，所述芳氧基本身也可被一个或两个取代基选自卤素原子和1至4个碳原子的烷基取代，以及其药学上可接受的酸加盐。还公开了制备这些化合物的过程，含有它们的制药组合物以及一种恢复温血动物的异常精神状态的方法。