(3,4-二氯苄基)-肼 | 51421-15-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: (3,4-二氯苄基)-肼
• 英文名称: 3,4-Dichlor-benzylhydrazin
• 英文别名: (3,4-Dichlorobenzyl)hydrazine；(3,4-dichlorophenyl)methylhydrazine
• CAS: 51421-15-9
• 化学式: C₇H₈Cl₂N₂
• mdl: MFCD27756467
• 分子量: 191.06
• InChiKey: OMBMILBFFMGAJD-UHFFFAOYSA-N

物化性质

• 沸点：
  112-116 °C(Press: 0.6 Torr)
• 密度：
  1.344±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  38
• 氢给体数：
  2
• 氢受体数：
  2

安全信息

• 海关编码：
  2928000090

反应信息

• 作为反应物：
  描述：

  (3,4-二氯苄基)-肼 在 硫酸 、 potassium hydroxide 、 三氯氧磷 作用下， 以 乙醇 为溶剂， 反应 22.0h， 生成 (E)-3-(1-(3,4-dichlorobenzyl)-3-(4-fluorophenyl)-1H-pyrazol-4-yl)-1-(4-fluoro-2-hydroxyphenyl)prop-2-en-1-one
  参考文献：
  名称：

  新型2-（1-苄基-3-3- [4-氟苯基] -1H-吡唑-4-基）-7-氟-4H-铬-4-基衍生物的合成与表征

  摘要：

  通过适当的1-苄基-2-（1-（4-氟苯基）亚乙基）的Vilsmeier-Haack反应合成了新颖的1-苄基-3-（4-氟苯基）-1 H-吡唑-4-甲醛3a至3e衍生自4-氟苯乙酮1的2-肼苯并肼2a至2e。1-苄基-3-（4-氟苯基）-1 H-吡唑-4-甲醛3a至3e与1-（4-氟-2-羟基苯基）乙酮4的碱催化缩合得到（E）-3-（ 1-苄基-3-（4-氟苯基）-1 H-吡唑-4-基）-1-（4-氟-2-羟苯基）丙-2-烯-1-酮5a到5e。在用二甲亚砜（DMSO）/ I 2环化时，化合物5a至5e得到2-（1-苄基-3-（4-氟苯基）-1 H-吡唑-4-基）-7-氟-4 H-色烯‐4‐one 6a至6e。所有新化合物的结构均通过红外（IR），质子核磁共振（1 H NMR），碳核磁共振（13 C NMR）和质谱数据证实。筛选所有合成的化合物的抗菌活性。

  DOI：

  10.1002/jhet.3894
• 作为产物：
  描述：

  3,4-二氯氯苄 在 一水合肼 作用下， 以 乙醇 为溶剂， 生成 (3,4-二氯苄基)-肼
  参考文献：
  名称：

  Iorio,M.A.; Landi Vittory,R., Farmaco, Edizione Scientifica, 1963, vol. 18, p. 453 - 464

  摘要：

  DOI：

文献信息

• ADENOSINE A2A RECEPTOR ANTAGONISTS
  申请人：Clasby Martin C.

  公开号：US20080255156A1

  公开（公告）日：2008-10-16

  Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein: X 1 and X 2 are 1-3 substituents independently selected from the group consisting of H, alkyl, halo, —CF 3 , —OCF 3 , alkoxy, —OH and —CN; n is 0, 1 or 2; and R and R 1 are H or alkyl; also disclosed is the use of the compounds in the treatment of CNS diseases such as Parkinson's disease, alone or in combination with other agents for treating CNS diseases, pharmaceutical compositions comprising them and kits comprising the components of the combinations.

  具有结构式I或其药用可接受盐的化合物，其中：X1和X2分别选自H、烷基、卤、—CF3、—OCF3、烷氧基、—OH和—CN组成的1-3个取代基；n为0、1或2；R和R1为H或烷基；还公开了该化合物在治疗中枢神经系统疾病如帕金森病中的用途，单独或与其他治疗中枢神经系统疾病的药剂联合使用，包括它们的药物组合物和包含该组合物成分的工具包。
• 1-Substituted-3-amino-pyrazol-5-ones
  申请人：Bayer Aktiengesellschaft

  公开号：US03950528A1

  公开（公告）日：1976-04-13

  Pharmaceutical compositions are prepared which comprise a diuretically effective amount, a saluretically effect amount or an antihypertensive amount of a compound of the formula ##SPC1## Or a pharmaceutically acceptable non-toxic salt thereof, wherein R is aryl which is either unsubstituted or substituted by A. 1, 2 or 3 identical or different substituents selected from the group consisting of halogen, alkyl of 1 to 8 carbon atoms, alkoxy of 1 to 8 carbon atoms, alkenoxy of 2 to 6 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, trifluoromethyl, trifluoromethoxy and phenyl; B. 1 or 2 identical or different substituents selected from the group consisting of nitro, cyano, lower alkylamino of 1 to 4 carbon atoms, a carbonamido moiety of the formula ##EQU1## and a sulphonamido moiety of the formula ##EQU2## wherein R.sub.1 and R.sub.2 are each hydrogen or straight or branched chain alkyl of 1 to 4 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are linked together to form a 5-, 6- or 7-membered heterocyclic ring wherein the nitrogen atom is the only heteroatom or wherein oxygen is also present as a ring member; C. one substituent selected from the group consisting of dialkylamino of 1 to 4 carbon atoms in each alkyl moiety, nitro, cyano and SO.sub.n -alkyl of 1 to 4 carbon atoms, wherein n is 0, 1 or 2; D. one substituent selected from the group consisting of a moiety of the formula ##EQU3## wherein R.sub.1 and R.sub.2 are as above defined, nitro, cyano, a carbonamido moiety of the formula ##EQU4## wherein R.sub.1 and R.sub.2 are as above defined, a sulphonamide moiety of the formula ##EQU5## wherein R.sub.1 and R.sub.2 are as above defined, and SO.sub.n -alkyl of 1 to 4 carbon atoms, wherein n is 0, 1 or 2, and 1 or 2 substituents selected from the group consisting of alkyl of 1 to 8 carbon atoms, alkoxy of 1 to 6 carbon atoms, halogen and trifluoromethyl; E. an annellated-branched or unbranched, saturated or unsaturated, 5-, 6- or 7-membered isocyclic or heterocyclic ring having 1 or more heteroatoms selected from the group consisting of oxygen and sulphur and wherein said aryl moiety is either unsubstituted or chlorosubstituted; F. --O--(CH.sub.2).sub.n.sub.' --N(alkyl).sub.2, wherein the alkyl groups contain a total of 2 to 4 carbon atoms and n'is 2 or 3; or G. two different substituents selected from the group consisting of alkyl of 1 to 8 carbon atoms, phenyl, halogen, alkoxy of 1 to 8 carbon atoms, trifluoromethyl, trifluoromethoxy, lower alkylamino, nitro, cyano, SO.sub.n --alkyl of 1 to 4 carbon atoms, wherein n is 0, 1 or 2, a carbonamido moiety of the formula ##EQU6## and a sulphonamido moiety of the formula ##EQU7## wherein R.sub.3 and R.sub.4 are each hydrogen or alkyl of 1 to 4 carbon atoms; in combination with a pharmaceutically acceptable non-toxic inert diluent or carrier. Diuretic therapy, saluretic therapy and antihypertensive therapy is effected in humans and animals by administering an effective amount of the active ingredient as above defined.

  制备了药物组合物，其中包括一种利尿有效量、排盐有效量或抗高血压有效量的化合物，其化学结构如下：其中R是芳基，可以是未取代或由A取代的芳基，A是1、2或3个相同或不同的取代基，包括卤素、1至8个碳原子的烷基、1至8个碳原子的烷氧基、2至6个碳原子的烯氧基、5至7个碳原子的环烷基、三氟甲基、三氟甲氧基和苯基；B是1个或2个相同或不同的取代基，包括硝基、氰基、1至4个碳原子的较低烷基氨基、具有以下结构的羰基基团和具有以下结构的磺胺基团；C是来自以下群体的1个取代基，包括每个烷基基团中1至4个碳原子的二烷基氨基、硝基、氰基和1至4个碳原子的SO.sub.n-烷基，其中n为0、1或2；D是来自以下群体的1个取代基，包括具有以下结构的基团，其中R.sub.1和R.sub.2如上定义，硝基、氰基、具有以下结构的羰基基团，其中R.sub.1和R.sub.2如上定义，具有以下结构的磺胺基团，其中R.sub.1和R.sub.2如上定义，以及1至4个碳原子的SO.sub.n-烷基，其中n为0、1或2，以及来自以下群体的1个或2个取代基，包括1至8个碳原子的烷基、1至6个碳原子的烷氧基、卤素和三氟甲基；E是一个具有1个或多个氧和硫异原子的芳基取代或氯取代的芳基，其中芳基可以是环状分支或非分支、饱和或不饱和、5、6或7个成员的异环或杂环，F是--O--(CH.sub.2).sub.n' --N(烷基).sub.2，其中烷基基团总共含有2至4个碳原子，n'为2或3；或G是来自以下群体的两个不同的取代基，包括1至8个碳原子的烷基、苯基、卤素、1至8个碳原子的烷氧基、三氟甲基、三氟甲氧基、较低烷基氨基、硝基、氰基、1至4个碳原子的SO.sub.n-烷基，其中n为0、1或2，具有以下结构的羰基基团和具有以下结构的磺胺基团，其中R.sub.3和R.sub.4分别是氢或1至4个碳原子的烷基；与药学上可接受的无毒惰性稀释剂或载体结合。通常通过给人类和动物使用上述定义的活性成分的有效量来进行利尿疗法、排盐疗法和抗高血压疗法。
• Pyrazol-5-ones
  申请人：Bayer Aktiengesellschaft

  公开号：US03949083A1

  公开（公告）日：1976-04-06

  Pharmaceutical compositions useful for effecting diuresis and saluresis and for treating hypertension in humans and animals are produced by combining a pyrazol-5-one of the formula: ##SPC1## Or a pharmaceutically acceptable nontoxic salt thereof wherein R is hydrogen, lower alkyl or amino; R.sup.1 is lower alkyl, alkenyl of 2 to 4 carbon atoms, monoaryl or monoaralkyl unsubstituted or substituted in the aryl moiety by 1 or 2 of the same or different substituents selected from the group consisting of lower alkyl, lower alkenyl, lower alkoxy, lower alkenoxy, halogen, nitro, cyano and trifluoromethyl; X is methylene, ethylene, methylene wherein 1 hydrogen atom is substituted by lower alkyl, or ethylene wherein 1 hydrogen atom is substituted by lower alkyl or 1 hydrogen atom on each of the two carbon atoms is substituted by lower alkyl; Y is a direct bond, oxygen or sulphur, provided that when X is methylene, Y is a direct bond; and Z is aryl unsubstituted or nuclear substituted by: A. 3 halogens; B. 1 or 2 of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, lower alkyl, lower alkenyl, lower alkoxy, lower alkenoxy, cycloalkyl of 5 to 7 carbon atoms and cycloalkenyl of 5 to 7 carbon atoms; C. lower alkylamino, dilower alkylamino, trifluoromethoxy, nitro, cyano, carbamoyl, lower alkylcarbamoyl, dilower alkylcarbamoyl, sulphamyl, lower alkylsulphamyl, dilower alkylsulphamyl, or --SO.sub.n --lower alkyl wherein n is 0, 1 or 2; D. lower alkylamino, dilower alkylamino, trifluoromethoxy, nitro, cyano, carbamoyl, lower alkylcarbamoyl, dilower alkylcarbamoyl, sulphamyl, lower alkylsulphamyl, dilower alkylsulphamyl, or --SO.sub.n --lower alkyl wherein n is 0, 1 or 2, and 1 or 2 of the same or different substituents selected from the group consisting of lower alkyl, lower alkenyl, lower alkoxy, halogen, and trifluoromethyl; E. dilower alkylamino, carbamoyl, lower alkylcarbamoyl, dilower alkylcarbamoyl, sulphamyl, lower alkylsulphamyl, or dilower alkylsulphamyl wherein the nitrogen atom is a member of 5-, 6- or 7-membered heterocyclic ring or said ring which contains oxygen as an additional ring member; or F. a fused, saturated or unsaturated 5-, 6- or 7-membered ring or said ring which additionally contains 1 or 2 oxygen atoms or 1 sulphur atom, With a pharmaceutically acceptable nontoxic inert diluent or carrier. The compositions are preferably administered orally or parenterally and in the latter case, sterile or isotonic aqueous solutions are preferred.

  用于促进人类和动物的利尿和盐利尿以及治疗高血压的制药组合物，通过将式为：##SPC1## 或其药学上可接受的无毒盐与惰性稀释剂或载体结合而制备。其中，R为氢、低碳基或氨基；R.sup.1为低碳基、2至4个碳原子的烯基、未取代或取代苯基或苯基烷基，所述苯基取代物为1或2个相同或不同的取代基，所述取代基为低碳基、低碳烯基、低碳氧基、低碳烯氧基、卤素、硝基、氰基和三氟甲基；X为亚甲基、乙烯基、其中1个氢原子被低碳基取代的亚甲基，或其中两个碳原子上的每个氢原子均被低碳基取代的乙烯基；Y为直接键、氧或硫，但当X为亚甲基时，Y为直接键；Z为未取代或核取代的苯基，所述取代物为：A. 3个卤素；B. 1或2个相同或不同的取代基，所述取代基为卤素、三氟甲基、低碳基、低碳烯基、低碳氧基、低碳烯氧基、5至7个碳原子的环烷基和5至7个碳原子的环烯基；C. 低碳基氨基、二低碳基氨基、三氟甲氧基、硝基、氰基、氨基甲酰基、低碳基氨基甲酰基、二低碳基氨基甲酰基、磺酰氨基、低碳基磺酰氨基、二低碳基磺酰氨基或--SO.sub.n--低碳基，其中n为0、1或2；D. 低碳基氨基、二低碳基氨基、三氟甲氧基、硝基、氰基、氨基甲酰基、低碳基氨基甲酰基、二低碳基氨基甲酰基、磺酰氨基、低碳基磺酰氨基、二低碳基磺酰氨基或--SO.sub.n--低碳基，其中n为0、1或2，且1或2个相同或不同的取代基为低碳基、低碳烯基、低碳氧基、卤素和三氟甲基；E. 二低碳基氨基、氨基甲酰基、低碳基氨基甲酰基、二低碳基氨基甲酰基、磺酰氨基、低碳基磺酰氨基、二低碳基磺酰氨基或二低碳基磺酰氨基，其中氮原子是5、6或7元杂环环或含氧作为附加环成员的所述环；或F. 融合的、饱和或不饱和的5、6或7元杂环环或含1或2个氧原子或1个硫原子的所述环，该组合物最好通过口服或肠外给药，并且在后一种情况下，最好使用无菌或等渗的水溶液。
• Miniature rose plant named ‘KORaroma07’
  申请人：W. Kordes Söhne Rosenschulen GmbH & Co. KG

  公开号：USPP030420P3

  公开（公告）日：2019-04-23

  ‘KORaroma07’ is a new and distinct variety of Rosa hybrida plant which is characterized by the combination of a compact and bushy growth habit with a moderately vigorous rate of growth, above average resistance to many rose diseases, pink flowers borne solitarily and in racemes of 2 to 5 flowers, double flowers, and flowers with a moderately strong myrrh and floral perfume. The new variety propagates successfully by stem cuttings and grafting and has shown to be uniform and stable in the resulting generations from asexual propagation.

  ‘KORaroma07’是一种新的、独特的玫瑰杂交植物品种，其特点是紧凑且灌木状的生长习性，生长速度适中，对许多玫瑰病害具有较高的抗性，花朵呈粉色，单独或成2至5朵的聚伞花序，双层花瓣，花香带有适度强烈的没药和花香味。这个新品种可以通过茎插和嫁接成功繁殖，并且从无性繁殖的结果世代中表现出均匀稳定的特性。
• Enzyme inhibitory phthalazin-4-ylacetic acid derivatives, pharmaceutical compositions thereof, and process for their manufacture
  申请人：IMPERIAL CHEMICAL INDUSTRIES PLC

  公开号：EP0002895A1

  公开（公告）日：1979-07-11

  This invention relates to enzyme inhibitory, novel phthalazin-4-ylacetic acid derivatives of the general formula wherein R1 is a hydroxy or benzyloxy radical, or a C1-4- alkoxy radical optionally bearing an N-morpholino or a C1-4-alkylamino radical, X is oxygen or sulfur, the rings A and B may be substituted, pharmaceutically acceptable salts as appropriate, to pharmaceutical compositions thereof, and to analogy processes for their manufacture. The compounds of formula I are inhibitors of the enzyme aldose reductase in vivo and as such may be useful in the reduction or prevention of the development of the peripheral effects such as macular oedema, cataract, retinopathy or impaired neural conduction. A preferred compound is 2-(2-fluoro-4-bromobenzyl)-1,2-dihydro-1-oxophthalazin-4- ylacetic acid.

  本发明涉及通式如下的酶抑制性新型酞嗪-4-基乙酸衍生物 其中 R1 是羟基或苄氧基，或 C1-4-烷氧基，可选带有 N-吗啉基或 C1-4-烷基氨基，X 是氧或硫，环 A 和 B 可被取代，适当的药学上可接受的盐，其药物组合物，以及生产它们的类比工艺。式 I 的化合物是体内醛糖还原酶的抑制剂，因此可用于减少或预防黄斑水肿、白内障、视网膜病变或神经传导受损等外周效应的发生。一种优选化合物是 2-（2-氟-4-溴苄基）-1,2-二氢-1-氧代酞嗪-4-乙酸。